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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-SR144528
SR144528

Chemical Structure : SR144528

CAS No.: 192703-06-3

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SR144528 (SR-144528, SR 144528)

货号: PC-60753Not For Human Use, Lab Use Only.

SR144528 is a highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.

规格 价格 库存 数量
5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥3980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SR144528 is a highly potent, selective and orally active antagonist of CB2 receptor with Ki of 0.6 nM.
SR144528 displays 700-fold lower affinity (Ki= 400 nM) for CB1 receptors, and no affinity for any of the more than 70 receptors, ion channels or enzymes (IC50>10 uM).
SR144528 antagonizes the inhibitory effects of CP 55,940 on forskolin-stimulated adenylyl cyclase activity with EC50 of 10 nM in cell-based assays, selectively blocks the MAPK activity induced by CP 55,940 with IC50 of 39 nM.
SR144528 displaces the ex vivo [3H]-CP 55,940 binding to mouse spleen membranes (ED50=0.35 mg/kg) with a long duration of action.

物理化学性质&存储条件

分子量 476.05
分子式 C29H34ClN3O
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-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide

参考文献

1. Rinaldi-Carmona M, et al. J Pharmacol Exp Ther. 1998 Feb;284(2):644-50.

2. Portier M, et al. J Pharmacol Exp Ther. 1999 Feb;288(2):582-9.

3. Carayon P, et al. Blood. 1998 Nov 15;92(10):3605-15.

4. Griffin G, et al. Eur J Pharmacol. 1999 Jul 14;377(1):117-25.

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