BIM-46187 (hydrochloride)

BIM-46187 is an inhibitor of heterotrimeric G-protein signaling. It inhibits signaling through Galphai, Galphas, and Galphaq in MZ7 cells but selectively inhibits Galphaq in HEK293 and CHO cells, indicating cell-dependent inhibition. BIM-46187 (0.1-1 mg/kg) increases the paw withdrawal threshold to a mechanical stimulus in a rat model of carrageenan-induced hyperalgesia. 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.Formal Name: (2R,2'R)-3,3'-dithiobis[2-amino-1-[(8S)-8-(cyclohexylmethyl)-5,6-dihydro-2-phenylimidazo[1,2-a]pyrazin-7(8H)-yl]-1-propanone, tetrahydrochloride. CAS Number: 2489449-03-6. Molecular Formula: C44H58N8O2S2 . 4HCl. Formula Weight: 941.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 260 nm. 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. InChi Code: InChI=1S/C44H58N8O2S2.4ClH/c45-35(43(53)51-23-21-49-27-37(33-17-9-3-10-18-33)47-41(49)39(51)25-31-13-5-1-6-14-31)29-55-56-30-36(46)44(54)52-24-22-50-28-38(34-19-11-4-12-20-34)48-42(50)40(52)26-32-15-7-2-8-16-32,,,,/h3-4,9-12,17-20,27-28,31-32,35-36,39-40H,1-2,5-8,13-16,21-26,29-30,45-46H2,4*1H/t35-,36-,39-,40-,,,,/m0..../s1. InChi Key: RKTRULIWGAJVGM-FPBFTDTKSA-N.