产品
编 号:F194864
分子式:C21H21N3O4
分子量:379.41
产品类型
结构图
CAS No: 1623481-80-0
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生物活性:
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
体内研究:
ML381 (0.2 mg/kg; i.v.; single) 在大鼠药效学研究中具有总体可接受的 DMPK 特征,但代谢稳定性差,且在血浆中可能发生酰胺水解;因此最适合作为体外/电生理探针使用。Animal Model:Sprague-Dawley rat.
Dosage:0.2 mg/kg
Administration:Intravenous injection; single.
Result:1.19Pharmacokinetic Parameters of ML381 in Sprague-Dawley rat.IV (0.2 mg/kg)
Hepatic microsomal CLint (mL min-1 kg-1)770
Predicted CLhep (mL min-1 kg-1)64
fubrain0.14
Cbrain/Cplasma (Kp*)0.58
*Kp value was determined at 0.25 h following a 0.2 mg/kg IV dose (n=2).