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Clemastine Fumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Clemastine Fumarate图片
CAS NO:14976-57-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Clemastine (HS-592) fumarate 是一种选择性组胺 H1 受体拮抗剂。
Cas No.14976-57-9
别名富马酸氯马斯汀; HS-592 fumarate; Meclastine fumarate
化学名(E)-but-2-enedioic acid;(2R)-2-[2-[(1R)-1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidine
Canonical SMILESCC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCC3CCCN3C.C(=CC(=O)O)C(=O)O
分子式C21H26ClNO.C4H4O4
分子量459.96
溶解度≥ 11.5mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Clemastine (fumarate) (HS-592 (fumarate)) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

Clemastine (fumarate) (HS-592 (fumarate)) inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively[1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, 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 consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race[2].

References:
[1]. Seifert, R., et al., Histamine increases cytosolic Ca2+ in dibutyryl-cAMP-differentiated HL-60 cells via H1 receptors and is an incomplete secretagogue. 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 and combination formulations. J Clin Pharmacol, 1996. 36(10): p. 911-22.