GPR81 agonist 1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 EC50s 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.

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Animal Model:Nine-week-old male C57/Bl6 mice (fed and fasted mice)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 Dosage:10 mg/kg (Pharmacokinetic Analysis) Administration:I.p.(Pharmacokinetic Analysis)Result:Showed good bioavailability (71%) and Cmax (6.3 μM).

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Cell Cycle/DNA Damage

GPR

GPR

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1620992-67-7

446.63

C22H30N4O2S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (111.95 mM; 超声助溶 )

C[C@H]1CC[C@@H](CC1)C(=O)Nc1nc(c(CC(=O)N2CCN(C)CC2)s1)-c1cccs1

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(-20℃)

With Ice Pack

≥ 2 years