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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-SR141716
SR141716

Chemical Structure : SR141716

CAS No.: 168273-06-1

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SR141716 (Rimonabant, SR141617, SR141716A)

货号: PC-22188Not For Human Use, Lab Use Only.

Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with Ki of 1.8 nM, no affinity for peripheral cannabinoid receptor.

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25 mg ￥980 In stock
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100 mg ￥2280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with Ki of 1.8 nM, no affinity for peripheral cannabinoid receptor.
Rimonabant (SR141716) antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and dopamine-stimulated adenylyl cyclase activities in rat brain membranes.
After oral administration Rimonabant (SR141716) totally inhibited the ex vivo [3H]-CP55,940 binding to cerebral membranes with a ED50 value of 3.5 mg/kg.
Rimonabant (SR141716) antagonizes the classical pharmacological responses elicited by cannabinoid receptor agonists.
Rimonabant (SR141716) reverses the inhibitory effect of WIN55212-2 on isoniazid-induced elevation of cGMP in rat cerebellum.

物理化学性质&存储条件

分子量 463.79
分子式 C22H21Cl3N4O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

参考文献

1. Yaksh TL, et al. J Pharmacol Exp Ther. 2006 Jan;316(1):466-75.

2. Rinaldi-Carmona M, et al. FEBS Lett. 1994 Aug 22;350(2-3):240-4.

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