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Clobenpropit dihydrobromide
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。
Clobenpropit dihydrobromide图片
CAS NO:145231-35-2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Clobenpropit dihydrobromide 是一种有效的组胺 H3R 拮抗剂/反向激动剂,组胺 H3LR 的 pEC50 为 8.07。
Cas No.145231-35-2
别名丙酸倍氯松二溴酸盐溶液,1000PPM,VUF 9153
化学名(Z)-3-(1H-imidazol-5-yl)propyl N'-4-chlorobenzylcarbamimidothioate dihydrobromide
Canonical SMILESClC1=CC=C(C=C1)C/N=C(N)\SCCCC2=CN=CN2.Br.Br
分子式C14H17ClN4S.2HBr
分子量470.65
溶解度30 mg/ml in DMSO, 2.5 mg/ml in Ethanol, 20 mg/ml in water
储存条件Store at -20℃
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

Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes).[1] Clobenpropit (0.3, 0.1, and 3 nM) reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by the H3 receptor agonist (R)-α-methylhistamine. It does not inhibit histamine-induced contractions in isolated guinea pig ileum or tachycardia in isolated right atria at concentrations up to 1 μM, indicating a lack of functional antagonist activity at H1 and H2 receptors, respectively. Clobenpropit (1 and 3 mg/kg) decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice, an effect that can be blocked by (R)-α-methylhistamine or imetit.[2] Clobenpropit (0.1 μM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.[3]

Reference:
[1]. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature 472(7344), 491-494 (2011).
[2]. Yokoyama, H., Onodera, K., Maeyama, K., et al. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur. J. Pharmacol. 260(1), 23-28 (1994).
[3]. Dai, H., Fu, Q., Shen, Y., et al. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur. J. PHarmacol. 563(1-3), 117-123 (2007).