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BIM-46187(hydrochloride)
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。
BIM-46187(hydrochloride)图片
CAS NO:2489449-03-6
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
An inhibitor of heterotrimeric G-protein signaling
Cas No.2489449-03-6
Canonical SMILESO=C(N1[C@H](C2=NC(C3=CC=CC=C3)=CN2CC1)CC4CCCCC4)[C@@H](N)CSSC[C@H](N)C(N5CCN6C([C@@H]5CC7CCCCC7)=NC(C8=CC=CC=C8)=C6)=O.Cl.Cl.Cl.Cl
分子式C44H58N8O2S2·4HCl
分子量941
溶解度DMF: 30 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
储存条件-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

BIM-46187 is an inhibitor of heterotrimeric G-protein signaling.1,2It inhibits signaling through Gαi, Gαs, and Gαqin MZ7 cells but selectively inhibits Gαqin HEK293 and CHO cells, indicating cell-dependent inhibition.1BIM-46187 (0.1-1 mg/kg) increases the paw withdrawal threshold to a mechanical stimulus in a rat model of carrageenan-induced hyperalgesia.3It also reduces mechanical hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI) when administered at doses ranging from 0.3 to 3 mg/kg.

1.Schmitz, A.-L., Schrage, R., Gaffal, E., et al.A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformationChem. Biol.21(7)890-902(2014) 2.Zhang, H., Nielsen, A.L., and StrØmgaard, K.Recent achievements in developing selective Gq inhibitorsMed. Res. Rev.40(1)135-157(2019) 3.Favre-Guilmard, C., Zeroual-Hide, H., Soulard, C., et al.The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphineEur. J. Pharmacol.594(1-3)70-76(2008)