An inhibitor of heterotrimeric G-protein signaling
货号:ajcx25562
CAS:2489449-03-6
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
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BIM-46187 is an inhibitor of heterotrimeric G-protein signaling.^1,2It inhibits signaling through Gα_i, Gα_s, and Gα_qin MZ7 cells but selectively inhibits Gα_qin 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)