GPR81agonist1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58nM和50nM。GPR81agonist1抑制分化的3T3-L1脂肪细胞的脂解。GPR81agonist1抑制小鼠的脂解并不会造成皮肤潮红。GPR81agonist1对GPR81的选择性高于GPR109a。
货号:ajcx32134
CAS:1620992-67-7
分子式:C22H30N4O2S2
分子量：446.63
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[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 Cmax (6.3 μM)[1]. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice)[1]

[1]. Sakurai T, et al. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing. Eur J Pharmacol. 2014;727:1-7.