Clemastine-fumarate-HS-592-fumarate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEClemastine fumarateCat. No.: HY-B0298ACAS No.: 14976-57-9Synonyms: HS-592 (fumarate); Meclastine (fumarate)分式: CHClNO分量: 459.96作靶点: Histamine Receptor; Autophagy作通路: GPCR/G Protein; Immunology/Inflammation; NeuronalSignaling; Au

2、tophagy储存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 14.29 mg/mL (31.07 mM; Need ultrasonic)H2O : 0.67 mg/mL (1.46 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1741 mL 10.8705 mL 21.7410 mL5 mM 0.4348 mL 2.1741 mL 4.3482 mL10 mM

3、 0.2174 mL 1.0871 mL 2.1741 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: 1.43 mg/mL (3.11 mM); Clear sol

4、ution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 1.43 mg/mL (3.11 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.43 mg/mL (3.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Clemastine (fumarate) (HS-592 (fumarate)是组胺

5、H1受体拮抗剂，IC50为 3 nM。IC50 & Target Histamine H1 Receptor 1.体外研究 Clemastine (fumarate) (HS-592 (fumarate) inhibits histamine induced rise in Ca2+i in HL-60 cells with anIC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and100 nM, respectively 1. Clemast

6、ine showed a first-pass reduction in the extent of absorption, with oralbioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the highvolume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26hours after admini

7、stration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistentwith linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or

8、 by race2.REFERENCES1. Seifert, R., et al., Histamine increases cytosolic Ca2+ in dibutyryl-cAMP-differentiated HL-60 cells via H1 receptors and is an incompletesecretagogue. Mol Pharmacol, 1992. 42(2): p. 227-34.2. Schran, H.F., et al., The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component andcombination formulations. J Clin Pharmacol, 1996. 36(10): p. 911-22.McePdfHeightCaution: Product has not been fully validated for medical applic