Clozapine-N-oxide - 5-HT Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEClozapine N-oxideCat. No.: HY-17366CAS No.: 34233-69-7分式: CHClNO分量: 342.82作靶点: 5-HT Receptor; Drug Metabolite作通路: GPCR/G Protein; Neuronal Signaling; MetabolicEnzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mo

2、nths-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (291.70 mM)Methanol : 28.6 mg/mL (83.43 mM)H2O : 1 mg/mL (2.92 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9170 mL 14.5849 mL 29.1698 mL5 mM 0.5834 mL 2.9170 mL 5.8340 mL10 mM 0.2917 mL 1.

3、4585 mL 2.9170 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.29 mM); Clear solution1/2 Maste

4、r of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.29 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Clozapine N-oxide (CNO)是抗精神病药物氯氮平的主要代谢产物。 Clozapine N-oxide是DREADD 系统的激动剂。IC50 & Target DREADD 1体内研究 After a single intraperitoneal (i.p.) in

5、jection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide(CNO) plasma levels peak at 15 min and are very low after 2 h. Acutely administered CNO can bemetabolically converted to Clozapine in other species such as human and guinea-pig. The metabolites thatmay form after chronic administrati

6、on of CNO to DREADD-expressing mice (or other species) have not beenstudied systematically. However, even if back-transformation to Clozapine occurs after chronic CNOadministration, it should be noted that Clozapine is a more potent (by 10-fold) DREADD agonist than CNOitself. Moreover, confounding b

7、iological effects of potential CNO metabolites can be easily identified byincluding both saline- and CNO-treated WT animals in a particular DREADD study. Despite the short plasmahalf-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing exper

8、imental animals are usually much longer (6-10 h). One possibility is that CNO tends toaccumulate in tissues, although other scenarios are also feasible 1. Using a general pharmacokinetic modelfor the interconversion process, the mean total clearances of Clozapine and Clozapine N-oxide (CNO) are28.45

9、 L/hr and 45.30 L/hr, respectively 2.户使本产品发表的科研献 Biol Psychiatry. 2017 May 1;81(9):737-747. Proc Natl Acad Sci U S A. 2019 Jul 29. Neuropharmacology. 2018 Jun;135:474-486. Neuroscience. 2019 Jun 7. pii: S0306-4522(19)30357-4. University of Michigan, Horace H. Rackham School of Graduate Studies. 2018

10、 Oct.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34(7):385-92.2. Chang WH, et al. Reversible metabolism of clozapine and clozapine N-oxide in schizophrenic patients. Prog NeuropsychopharmacolBiol Psychiatry. 1998 Jul;22(5):723-39.McePdfHeightCaution: Product has not been fully v