Horiguchi, M. et al. published their research in Behavioural Brain Research in 2013 | CAS: 112457-95-1

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate

Blonanserin reverses the phencyclidine (PCP)-induced impairment in novel object recognition (NOR) in rats: Role of indirect 5-HT1A partial agonism was written by Horiguchi, M.;Meltzer, H. Y.. And the article was included in Behavioural Brain Research in 2013.Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate This article mentions the following:

Blonanserin is an atypical antipsychotic drug (APD) which, compared to other atypical APDs, is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist. Comparing blonanserin with more broadly acting atypical APDs could be useful to test the contributions of actions at other monoamine receptors, e.g. 5-HT1A receptors, to the reversal of PCP-induced novel object recognition (NOR) deficit. In this study, we tested the effect of blonanserin alone, and in combination with 5-HT1A agents, on NOR deficit induced by subchronic treatment with the N-methyl-D-aspartate (NMDA) receptor antagonist, phencyclidine (PCP; 2 mg/kg), b.i.d., for 7 days. Blonanserin, 1 mg/kg, but not 0.3 mg/kg, improved the PCP-induced NOR deficit. However, at 1 mg/kg, object exploration was diminished. Co-administration of sub-EDs of blonanserin (0.3 mg/kg) and the 5-HT1A partial agonist, tandospirone (0.2 mg/kg), significantly reversed the NOR deficit without diminishing activity during the acquisition or retention periods. The combination of WAY100635 (0.6 mg/kg), a 5-HT1A antagonist, and blonanserin (1 mg/kg), also diminished object exploration which prevented assessment of the effect of this combination on NOR. WAY100635 (0.6 mg/kg) blocked the ameliorating effect of risperidone (0.1 mg/kg), another atypical APD with low affinity for 5-HT1A receptors, but did not impair exploration. These results suggest that blonansein and risperidone, atypical APDs which lack a direct action on 5-HT1A receptors require 5-HT1A receptor stimulation to reverse the subchronic PCP-induced NOR deficit and provide a support for clin. trial of blonanserin in combination with tandospirone to ameliorate cognitive impairment in schizophrenia and to have fewer side effects. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Safety of rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Tang, Xiaoqiong et al. published their research in BMC Microbiology in 2022 | CAS: 13292-46-1

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.COA of Formula: C43H58N4O12

Antibiotic resistance patterns of Helicobacter pylori strains isolated from the Tibet Autonomous Region, China was written by Tang, Xiaoqiong;Wang, Zhonghua;Shen, Yalin;Song, Xiaona;Benghezal, Mohammed;Marshall, Barry J.;Tang, Hong;Li, Hong. And the article was included in BMC Microbiology in 2022.COA of Formula: C43H58N4O12 This article mentions the following:

The prevalence of Helicobacter pylori antibiotic susceptibility in the Tibet Autonomous Region, China is not determined This study aimed to evaluate the antibiotic resistance patterns of H. pylori isolates there. A total of 153 (38.5%) H. pylori strains were successfully isolated from 397 patients in People’s Hospital of Tibet Autonomous Region, China. The overall resistance rates were as follows: clarithromycin (27.4%), levofloxacin (31.3%), metronidazole (86.2%), amoxicillin (15.6%), tetracycline (0%), furazolidone (0.6%), and rifampicin (73.2%). Only 2.0% of H. pylori isolates were susceptible to all tested antimicrobials, with mono resistance, dual resistance, triple resistance, quadruple resistance, and quintuple resistance being 18.3%, 44.4%, 18.3%, 12.4%, and 4.6%, resp. The resistance rates to levofloxacin (40.5%) and amoxicillin (21.5%) in strains isolated from female patients were significantly higher than those from male patients (21.6% and 9.5%, resp.). This study demonstrates high H. pylori resistance rates to clarithromycin, levofloxacin, metronidazole, and rifampicin, whereas moderate resistance to amoxicillin, and negligible resistant to tetracycline, and furazolidone in Tibet Autonomous Region, China. The high resistance to rifampicin warns further investigation of its derivative, rifabutin. In the experiment, the researchers used many compounds, for example, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1COA of Formula: C43H58N4O12).

8-(n-(4-methyl-1-piperazinyl)formidoyl)-rifomycins (cas: 13292-46-1) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.COA of Formula: C43H58N4O12

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Huang, Shiyang et al. published their research in Water Research in 2021 | CAS: 68-88-2

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol

Surface modification of nanofiltration membranes to improve the removal of organic micropollutants: Linking membrane characteristics to solute transmission was written by Huang, Shiyang;McDonald, James A.;Kuchel, Rhiannon P.;Khan, Stuart J.;Leslie, Greg;Tang, Chuyang Y.;Mansouri, Jaleh;Fane, Anthony G.. And the article was included in Water Research in 2021.Safety of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol This article mentions the following:

Surface modification of nanofiltration (NF) membranes has great potential to improve the removal of organic micropollutants (OMs) by NF membranes. This study used polydopamine (PDA) as a model coating to comprehensively link the changes in membrane properties with the changes in transmission of 34 OMs. The membrane characterization demonstrated that a thicker, denser, and more hydrophilic PDA coating can be achieved by increasing the PDA deposition time from 0.5 to 4 h. Overall, the transmissions of target OMs were reduced by PDA-coated NF membranes compared to unmodified NF membranes. The neutral hydrophobic compounds showed lower transmissions for longer PDA coating (PDA4), while the neutral hydrophilic compounds tended to show lower transmissions for shorter PDA coating (PDA0.5). To explain this, competing effects provided by the PDA coatings are proposed including sealing defects, inducing cake-enhanced concentration polarization in the coating layer for neutral hydrophilic compounds, and weakened hydrophobic adsorption for neutral hydrophobic compounds For charged compounds, PDA4 with the greatest neg. charge among the PDA-coated membranes showed the lowest transmission. Depending on the mol. size and hydrophilicity of the compounds, the transmission of OMs by the PDA4 coating could be reduced by 70% with only a 26.4% decline in water permeance. The correlations and mechanistic insights provided by this work are highly useful for designing membranes with sp. surface properties via surface modification to improve the removal of OMs without compromising water production In the experiment, the researchers used many compounds, for example, 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2Safety of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol).

2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol (cas: 68-88-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Safety of 2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)ethanol

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Sun, Yanying et al. published their research in European Journal of Medicinal Chemistry in 2021 | CAS: 304897-49-2

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket was written by Sun, Yanying;Kang, Dongwei;Da, Feng;Zhang, Tao;Li, Pei;Zhang, Baodan;De Clercq, Erik;Pannecouque, Christophe;Zhan, Peng;Liu, Xinyong. And the article was included in European Journal of Medicinal Chemistry in 2021.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate This article mentions the following:

With our previously identified potent NNRTIs 25a and HBS-11c as leads, series of novel thiophene[3,2-d]pyrimidine and thiophene[2,3-d]pyrimidine derivatives were designed via mol. hybridization strategy. All the target compounds were evaluated for their anti-HIV-1 activity and cytotoxicity in MT-4 cells. Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007渭M to 0.043渭M. Gratifyingly, 16b1 exhibited significantly reduced cytotoxicity (CC50 > 217.5渭M) and improved water solubility (S = 49.3渭g/mL at pH 7.0) compared to the lead 25a (S < 1渭g/mL at pH 7.0, CC50 = 2.30渭M). Moreover, mol. docking was also conducted to rationalize the structure-activity relationships of these novel derivatives and to understand their key interactions with the binding pocket. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate).

tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate (cas: 304897-49-2) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.Application In Synthesis of tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Natsui, Kiyohi et al. published their research in European Journal of Drug Metabolism and Pharmacokinetics in 2007 | CAS: 112457-95-1

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Synthetic Route of C27H37N5O9

Identification of CYP3A4 as the primary cytochrome P450 responsible for the metabolism of tandospirone by human liver microsomes was written by Natsui, Kiyohi;Mizuno, Yoshiko;Tani, Naoko;Yabuki, Masashi;Komuro, Setsuko. And the article was included in European Journal of Drug Metabolism and Pharmacokinetics in 2007.Synthetic Route of C27H37N5O9 This article mentions the following:

The present study was carried out to characterize the human P 450 isoforms involved in the metabolism of tandospirone, an anxiolytic agent known for its superior efficacy and safety. Among 11 yeast-expressed recombinant P 450 isoforms tested, CYP2D6 and CYP3A4 exhibited the highest tandospirone metabolic activity. Although there was no qual. difference between the two isoforms, a quant. difference in metabolite profiling was found i.e., M4 (hydroxylation of the pyrimidine ring) was the major metabolite formed with CYP2D6 while M2 (hydroxylation of the norbornan ring) and 1-PP (oxidative cleavage of the Bu chain) predominated with CYP3A4. The metabolite profile on incubation with CYP3A4 was qual. and quant. similar to that obtained with human liver microsomes. In vitro intrinsic clearance (CLint) values derived from kinetic anal. using both P 450 isoforms were similar (2.2 and 1.6 mL/min/nmol P 450), but the hepatic content of CYP3A4 was found to be more abundant than that of CYP2D6. The in vitro metabolism of tandospirone by human liver microsomes was markedly inhibited by ketoconazole (a CYP3A4 inhibitor) but not by quinidine (a CYP2D6 inhibitor). These results indicate that the metabolism of tandospirone by human liver microsomes primarily involves CYP3A4, and to a lesser extent CYP2D6. In the experiment, the researchers used many compounds, for example, rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1Synthetic Route of C27H37N5O9).

rel-(3aR,4S,7R,7aS)-2-(4-(4-(Pyrimidin-2-yl)piperazin-1-yl)butyl)hexahydro-1H-4,7-methanoisoindole-1,3(2H)-dione 2-hydroxypropane-1,2,3-tricarboxylate (cas: 112457-95-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Synthetic Route of C27H37N5O9

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Mishra, Chandra Bhushan et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 27469-60-9

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.HPLC of Formula: 27469-60-9

Discovery of Benzenesulfonamide Derivatives as Carbonic Anhydrase Inhibitors with Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Evaluation was written by Mishra, Chandra Bhushan;Kumari, Shikha;Angeli, Andrea;Bua, Silvia;Tiwari, Manisha;Supuran, Claudiu T.. And the article was included in Journal of Medicinal Chemistry in 2018.HPLC of Formula: 27469-60-9 This article mentions the following:

Two series of novel benzenesulfonamide derivatives were synthesized and evaluated for their human carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity against four isoforms, hCA I, hCA II, hCA VII, and hCA IX. It was found that compounds of both series showed low to medium nanomolar inhibitory potential against all isoforms. Some of these derivatives displayed selective inhibition against the epileptogenesis related isoforms hCA II and VII, within the nanomolar range. These potent hCA II and VII inhibitors were evaluated as anticonvulsant agents against MES and s.c.-PTZ induced convulsions. These sulfonamides effectively abolished induced seizures in both models. Furthermore, time dependent seizure protection capability of the most potent compound I was also evaluated. A long duration of action was displayed, with efficacy up to 6 h after drug administration. The compound appeared as an orally active anticonvulsant agent without showing neurotoxicity in a rotarod test, a nontoxic chem. profile being observed in subacute toxicity study. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).

4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine is formed as a co-product in the ammoniation of 1,2-dichloroethane or ethanolamine. These are the only routes to the chemical used commercially.HPLC of Formula: 27469-60-9

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Altaif, K. I. et al. published their research in American Journal of Veterinary Research in 1972 | CAS: 142-64-3

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Formula: C4H12Cl2N2

Comparative evaluation of efficacies of dl-tetramisole and piperazine against Ascaridia galli in chickens was written by Altaif, K. I.. And the article was included in American Journal of Veterinary Research in 1972.Formula: C4H12Cl2N2 This article mentions the following:

Dl-tetramisole (I) [5036-02-2] (20 and 40 mg/kg) administered in drinking water proved 87.7 and 99.0% efficacious, resp., against mature Ascaridia galli in chickens, whereas 20 mg/kg I mixed with feed gave a 63.0% reduction of the fecal egg count. Piperazine-2HCl [142-64-3] (260 mg/kg) given in drinking water resulted in a 96.4% reduction in fecal egg count whereas when given in the feed a 79.0% reduction was observed In the experiment, the researchers used many compounds, for example, Piperazine Dihydrochloride (cas: 142-64-3Formula: C4H12Cl2N2).

Piperazine Dihydrochloride (cas: 142-64-3) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Formula: C4H12Cl2N2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Cristinziano, Giulia et al. published their research in Journal of Hepatology in 2021 | CAS: 872511-34-7

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application of 872511-34-7

FGFR2 fusion proteins drive oncogenic transformation of mouse liver organoids towards cholangiocarcinoma was written by Cristinziano, Giulia;Porru, Manuela;Lamberti, Dante;Buglioni, Simonetta;Rollo, Francesca;Amoreo, Carla Azzurra;Manni, Isabella;Giannarelli, Diana;Cristofoletti, Cristina;Russo, Giandomenico;Borad, Mitesh J.;Grazi, Gian Luca;Diodoro, Maria Grazia;Giordano, Silvia;Sacconi, Andrea;Forcato, Mattia;Anastasi, Sergio;Leonetti, Carlo;Segatto, Oreste. And the article was included in Journal of Hepatology in 2021.Application of 872511-34-7 This article mentions the following:

About 15% of intrahepatic cholangiocarcinomas (iCCAs) express fibroblast growth factor receptor 2 (FGFR2) fusion proteins (FFs), usually alongside mutational inactivation of TP53, CDKN2A or BAP1. In FFs, FGFR2 residues 1-768 fuse to sequences encoded by a diverse array of partner genes (>60) causing oncogenic FF activation. While FGFR-specific tyrosine kinase inhibitors (F-TKI) provide clin. benefit in FF+ iCCA, responses are partial and/or limited by resistance mechanisms, such as the V565F substitution in the FGFR2 gatekeeper residue. Improving on FF targeting in iCCA therefore remains a critical unmet need. Herein, we aimed to generate a murine model of FF-driven iCCA and use this to uncover actionable FF-associated dependencies.Four iCCA FFs carrying different fusion sequences were expressed in Tp53-/- mouse liver organoids. Tumorigenic properties of genetically modified liver organoids were assessed by transplantation into immuno-deficient mice. Cellular models derived from neoplastic lesions were exploited for pre-clin. studies.Transplantation of FF-expressing liver organoids yielded tumors diagnosed as CCA based on histol., phenotypic and transcriptomic analyses. The penetrance of this tumorigenic phenotype was influenced by FF identity. Tumor organoids and 2D cell lines derived from CCA lesions were addicted to FF signaling via Ras-Erk, regardless of FF identity or V565F mutation. Dual blockade of FF and the Ras-Erk pathway by concomitant pharmacol. inhibition of FFs and Mek1/2 provided greater therapeutic efficacy than single agent F-TKI in vitro and in vivo.FF-driven iCCA pathogenesis was successfully modeled on a Tp53-/- murine background, revealing biol. heterogeneity among structurally different FFs. Double blockade of FF-ERK signaling deserves consideration for precision-based approaches against human FF+ iCCA.Intrahepatic cholangiocarcinoma (iCCA) is a rare cancer that is difficult to treat. A subtype of iCCA is caused by genomic alterations that generate oncogenic drivers known as FGFR2 fusions. Patients with FGFR2 fusions respond to FGFR inhibitors, but clin. responses are often of modest duration. We used animal and cellular models to show that FGFR2 fusions require the activity of a downstream effector named Mek1/2. We found that dual blockade of FGFR2 fusions and Mek1/2 was more effective than isolated inhibition of FGFR2 fusions, pointing to the potential clin. utility of dual FGFR2-MEK1/2 blockade in patients with iCCA. In the experiment, the researchers used many compounds, for example, 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7Application of 872511-34-7).

3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea (cas: 872511-34-7) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application of 872511-34-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Breton, Yann et al. published their research in Journal of Virology in 2019 | CAS: 548472-68-0

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one

Expression of MDM2 in macrophages promotes the early postentry steps of HIV-1 infection through inhibition of p53 was written by Breton, Yann;Desrosiers, Vincent;Ouellet, Michel;Deshiere, Alexandre;Torresilla, Cynthia;Cohen, Eric A.;Tremblay, Michel J.. And the article was included in Journal of Virology in 2019.Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one This article mentions the following:

The mol. basis for HIV-1 susceptibility in primary human monocyte-derived macrophages (MDMs) was previously evaluated by comparing the transcriptome of infected and bystander populations. In this study, MDM2 silencing through transcript-specific small interfering RNAs in MDMs induced a reduction in HIV-1 reverse transcription and integration along with an increase in the expression of p53-induced genes, including CDKN1A. Experiments with Nutlin-3, a pharmacol. inhibitor of MDM2 p53-binding activity, showed a similar effect on HIV-1 infection, suggesting that the observed restriction in HIV-1 production results from the release/activation of p53 and not the absence of MDM2 per se. IMPORTANCE Macrophages, with their long life span in vivo and their resistance to HIV-1-mediated cytopathic effect, might serve as viral reservoirs, contributing to virus persistence in an infected individual. Identification of host factors that increase the overall susceptibility of macrophages to HIV-1 might provide new therapeutic targets for the efficient control of viral replication in these cells and limit the formation of reservoirs in exposed individuals. In this study, we demonstrate the importance of p53 regulation by MDM2, which creates a cellular environment more favorable to the early steps of HIV-1 replication. Moreover, we show that p53 stabilization reduces virus infection in human macrophages, highlighting the important role of p53 in antiviral immunity. In the experiment, the researchers used many compounds, for example, 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one).

4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one (cas: 548472-68-0) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Application In Synthesis of 4-(cis-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hendrickson, O. D. et al. published their research in Journal of the Science of Food and Agriculture in 2019 | CAS: 113617-63-3

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C19H20F3N3O3

Development of a multicomponent immunochromatographic test system for the detection of fluoroquinolone and amphenicol antibiotics in dairy products was written by Hendrickson, O. D.;Zvereva, E. A.;Shanin, I. A.;Zherdev, A. V.;Dzantiev, B. B.. And the article was included in Journal of the Science of Food and Agriculture in 2019.Computed Properties of C19H20F3N3O3 This article mentions the following:

BACKGROUND : Ciprofloxacin (CIP) and chloramphenicol (CAP) are relevant antibiotics of the fluoroquinolone (FQ) and amphenicol (AP) groups, resp., widely used in veterinary practice and they contaminate agricultural products. In this study, a rapid and sensitive immunochromatog. assay (ICA) was developed for simultaneous detection of CIP and CAP in dairy products. The ICA was carried out in a direct competitive format using gold nanoparticles as a label. RESULTS : The ICA developed here allowed for the detection of CIP and CAP in Triton X-100-containing buffered saline (PBST) within 15 min with instrumental detection limits of 20 pg mL-1 and 0.5 ng mL-1, resp., and with a visual detection limit of 5 ng mL-1 for both antibiotics. The ICA showed cross-reactivity (69-160%) to 19 antibiotics in the FQ group and no cross-reactivity (<0.1%) to 2 antibiotics of the AP group. The ICA allowed detection of CIP and CAP in a panel of dairy products by employing a simple procedure of preliminary sample preparation The detection limits for the two antibiotics were the same as in PBST. The anal. recoveries of CIP and CAP in dairy products ranged from 83% to 120%. CONCLUSION : The anal. characteristics of the test system allow its use for the detection of antibiotics in milk and dairy products during all steps of production 漏 2019 Society of Chem. Industry. In the experiment, the researchers used many compounds, for example, 1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3Computed Properties of C19H20F3N3O3).

1-Cyclopropyl-7-(cis-3,5-dimethylpiperazin-1-yl)-5,6,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (cas: 113617-63-3) belongs to piperazine derivatives. Piperazine causes primary dermal irritation and skin burns at high concentrations. Piperazine also causes eye irritation in humans. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Computed Properties of C19H20F3N3O3

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics