CAS NO: | 2489449-03-6 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 2489449-03-6 |
Canonical SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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) |