Clozapine-N-oxide - 5-HT Receptor Antagonist - 生命科學試劑 - 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作靶點: 5-HT Receptor; Drug Metabolite作通路: GPCR/G Protein; Neuronal Signaling; MetabolicEnzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mo

2、nths-20C 1 month溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE2. 請依序添加每種溶劑： 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)是抗精神病藥物氯氮平的主要代謝產(chǎn)物。 Clozapine N-oxide是DREADD 系統(tǒng)的激動劑。IC50 & Target DREADD 1體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻 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