hGPR91 antagonist 1

Names

[ CAS No. ]:
1314796-00-3

[ Name ]:
hGPR91 antagonist 1

Biological Activity

[Description]:

HGPR91 antagonist 1 is a potent and selective small molecule hGPR91 antagonist with an IC50 of 7 μM[1].

[Related Catalog]:

Research Areas >> Others

Signaling Pathways >> Others >> Others

[Target]

IC50: 7 μM (HGPR91)[1]

[In Vivo]

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] Dosage: 100 mg/kg Administration: I.p.; 2 and 4 hours Result: Led to 59 and 76% inhibition of ΔMAP at 2 and 4 hours.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₁H₂₃F₄N₃O

[ Molecular Weight ]:
529.53

Related Compounds

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