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编 号:F746209
分子式:C22H30N4O2S2
分子量:446.63
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
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.

体内研究:
GPR81 激动剂 1 (100 mg/kg;腹腔注射) 抑制没有皮肤潮红的小鼠脂肪分解。GPR81 激动剂 1 (10 mg/kg;腹腔注射) 显示出良好的生物利用度 (71%) 和 Cmax (6.3 μM)。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).

体外研究:
GPR81 激动剂 1 (化合物 2) (1-1000 nM) 抑制分化的 3T3-L1 脂肪细胞中的脂肪分解。
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