GPR81 Agonist, 3Cl-5OH-BA - CAS 53984-36-4 - Calbiochem

A hydroxybenzoic acid compound that acts as a GPR81/HCA1-selective agonist (EC₅₀ ~ 7, 16, 17, 22, and 67 µM toward rat, human, monkey, mouse, and dog species, respectively) with little activity towards the homologous GPR109A/HCA2/HM74A GPCR (EC₅₀ >1 mM). Displays good pharmacokinetic characteristics in mice (C_max/t_1/2 = 67.2 µM/1.47 h and 341.9 µM/1.1 h, respectively, upon oral dosing at 30 mg/kg and 100 mg/kg) and exhibits NEFAc- (non-esterified free fatty acid cholesterol) lowering efficacy in overnight fasted C57B16/J mice (ED₅₀ ~100 mg/kg, p.o.) in vivo.

A hydroxybenzoic acid compound that acts as a GPR81/HCA1-selective agonist (EC₅₀ ~ 7, 16, 17, 22, and 67 µM toward rat, human, monkey, mouse, and dog species, respectively) with little activity towards the homologous GPR109A/HCA2/HM74A GPCR. Orally active in mice and exhibits NEFAc cholesterol-lowering efficacy in overnight fasted C57B16/J mice (ED₅₀ ~100 mg/kg, p.o.) in vivo.

Primary Target
GPR81

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Dvorak, C.A., et al. 2012. ACS Med. Chem. Lett.3, 637.

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