產品屬性：
產品名稱 | BIM-46187 (hydrochloride) |
規格 | 1 mg、5 mg、10 mg、25 mg |
貨號 | EY-01Y16703 |
Cas No.: 2489449-03-6
別名: N/A
化學名: N/A
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
儲存條件: -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
產品描述：
BIM-46187 is an inhibitor of heterotrimeric G-protein signaling.1,2 It inhibits signaling through Gαi, Gαs, and Gαq in MZ7 cells but selectively inhibits Gαq in HEK293 and CHO cells, indicating cell-dependent inhibition.1 BIM-46187 (0.1-1 mg/kg) increases the paw withdrawal threshold to a mechanical stimulus in a rat model of carrageenan-induced hyperalgesia.3 It 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 Str?mgaard, 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)
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