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CAS No. : 1488362-55-5
MCE 国际站:ML375
产品活性:ML375 (VU0483253) 是一种有效、高选择性、可透过血脑屏障和具有口服活性的 M5 mAChR 负变构调节剂 (NAM),对人和大鼠 M5 的 IC50 分别为 300 nM 和 790 nM。ML375 对人和大鼠的 M1-M4 无活性。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:mAChR
In Vitro: ML375 possesses high metabolic stability with low hepatic microsomal intrinsic clearance (CLint; human 2.6 mL/min/kg, cynomolgus monkey (cyno), 20 mL/min/kg, rat, 24 mL/min/kg) and a corresponding low predicted hepatic clearance in multiple species (CLhep; human, 2.3 mL/min/kg, cyno, 14 mL/min/kg rat, 18 mL/min/kg).
In Vivo: ML375 (10-30 mg/kg; i.p.; once) attenuates both the reinforcing effects and the relative strength of cocaine.
ML375 exhibits low clearance (CLp, 2.5 mL/min/kg) and a long elimination half-life (T1/2, 80 hr) in rodents (male, Sprague-Dawley rat, 1 mg/kg IV,) and nonhuman primates (male, cynomolgus monkey, 1 mg/kg, CLp, 3.0 mL/min/kg, T1/2, 10 hr).
ML375 also demonstrates high oral bioavailability (%F, 80) following administration of a suspension-dose to male SD rats with a maximal plasma concentration (Cmax) of 1.4 μM and a corresponding time to reach Cmax (Tmax) of 7 hours.
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货号: HY-12567
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