产品
编 号:F383969
分子式:C7H5ClO3
分子量:172.57
产品类型
结构图
CAS No: 53984-36-4
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产品详情
生物活性:
3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC50 of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity.
体内研究:
3-Chloro-5-hydroxybenzoic acid (30, 100, and 300 mg/kg; PO in overnight fasted C57Bl6/J mice fed high fat chow for 10 weeks) shows significant reductions in free fatty acids at all doses tested, resulting in a minimum efficacious dose of 30 mg/kg.Pharmacokinetic Parameters of 3-Chloro-5-hydroxybenzoic acid in Mice.dose (mg/kg)tmax (h) AUCinf (h ng/mL) Cmax (ng/mL) Cmax (μM)t1/2 (h)
30 0.5 9356 11689.50 67.2 1.47
100 0.5 51312 55252.80 341.9 1.10
Animal Model:C57Bl6/J mice (DIO mice)
Dosage:30, 100, and 300 mg/kg
Administration:PO in overnight fasted C57Bl6/J mice fed high fat chow for 10 weeks
Result:Significant reductions in nonesterified free fatty acid cholesterol (NEFAc) at all doses tested.
体外研究:
3-Chloro-5-hydroxybenzoic acid shows potency against human (EC50=16 μM), monkey (EC50=17 μM), dog (EC50=67 μM), rat (EC50=7 μM), mouse (EC50=22 μM), and hamster GPR81 (EC50=27 μM).