MAO-B-IN-5 是一种有效的、选择性和具有口服活性的MAO-B抑制剂,IC50值为 0.204 μM。MAO-B-IN-5 在帕金森病 (PD) 中具有研究潜力。
产品描述
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC 50 of 0.204 μM. MAO-B-IN-5 has the research potential in Parkinson's disease (PD) [1].
体外活性
MAO-B-IN-5 (compound D0) (Sf9 cells) has inhibitory activities towards MAO with the IC 50 s of 34.190 μM and 0.204 μM for MAO-A and MAO-B, respectively [1].
体内活性
MAO-B-IN-5 (1 mg/kg, i.v.; 5 mg/kg, p.o.) exhibis oral bioavailability in rats (F=13.6%) [1]. Pharmacokinetic Parameters of MAO-B-IN-5 in SD rats [1]. Compound Route Dose (mg/kg) C max (ng/mL) AUC t (ng·h/mL) T 1/2 (h) Vss (h) Cl (mL/min/kg) F (%) D0 iv 1 809 347 0.37 1.11 47.1 / po 5 163 284 1.27 / / 16.3
Cas No.
849909-77-9
分子式
C19H21FN2O2
分子量
328.38
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years