HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM[1]. IC50: 7 μM (HGPR91)[1]
HGPR91 antagonist 1 leads to 59, 76% inhibition of δMAP at 2, 4 hours and has shown rat plasma protein binding 99%. HGPR91 antagonist 1 has engaged the target under the in vivo condition. HGPR91 antagonist 1 has clearance (CL) of 0.2 nmol/min/mg of RLM[1]. Animal Model: Wistar rats[1]
[1]. Bhuniya D, et al. Discovery of a potent and selective small molecule hGPR91 antagonist. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3596-602.