GPR81 agonist 1 是一种高效、高选择性的GPR81激动剂，对人和小鼠 GPR81 的EC50分别为 58 nM 和 50 nM。GPR81 agonist 1 抑制分化的 3T3-L1 脂肪细胞的脂解。GPR81 agonist 1 抑制小鼠的脂解并不会造成皮肤潮红。GPR81 agonist 1 对 GPR81 的选择性高于 GPR109a。

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC 50 s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a [1].

GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes [1].

GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing [1]. GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C max (6.3 μM) [1]. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice) [1] Dosage: 100 mg/kg Administration: I.p. Result: Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg. Animal Model: Male C57/Bl6 mice [1] Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: I.p.(Pharmacokinetic Analysis) Result: Showed good bioavailability (71%) and C max (6.3 μM).

1620992-67-7

C22H30N4O2S2

446.63

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years