产品
编 号:F756122
分子式:C29H27N5O
分子量:461.56
产品类型
结构图
CAS No: 2815263-05-7
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产品详情
生物活性:
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable.
体内研究:
GPR84 antagonist 3 (compound 42) (1 mg/kg (IV), 10 mg/kg (Orally); once) has a good elimination half-life (2.51 h), moderate rate of clearance, and bioavailability.Animal Model:Male C57BL/6J mice (n = 3)
Dosage:1 mg/kg (IV), 10 mg/kg (Orally)
Administration:IV, Orally; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of GPR84 antagonist 3 in Male C57BL/6J mice.IV (1 mg/kg) PO (10 mg/kg)
half-life (h)2.51 ± 6.55
CL (mL/min/kg)38.9 ± 13.9
Vss (L/kg)7.24 ± 9.2
C0 (ng/mL)394 ± 19.1
AUCall (ng/mL·h)420 ± 12.51590 ± 18.7
Tmax (h)1
Cmax (ng/mL)402 ± 31.8
F (%)36.8 ± 18.7
体外研究:
GPR84 antagonist 3 (compound 42) displays no ability to block the actions of the C3 fatty acid propionate at either FFAR2 or FFAR3 when tested at 10 μM