ML380,1627138-52-6

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ML380

CAS No. : 1627138-52-6

MCE 国际站：ML380

产品活性：ML380 是一种有效的，亚型选择性和可透过血脑屏障的 M5 mAChR 正变构调节剂 (PAM)，对人和大鼠 M5 的 EC₅₀ 值分别为 190 和 610 nM。ML380 对 M1 和 M3 mAChR 亚型具有中等选择性。ML380 可以增加 Ach 对 M5 mAChR 的亲和力。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mAChR

In Vitro: ML380 (0.01 nM-100 μM) robustly stimulates inositol phosphate (IP) accumulation and Ca²⁺ mobilization in CHO-hM₅ cells, with pEC₅₀s of 5.33 and 5.71, respectively.
ML380 (0.01-30 μM) increases the ACh-stimulated IP accumulation and Ca²⁺ mobilization in CHO-hM₅ cells.

In Vivo: ML380 (1 mg/kg; i.v.) displays high clearance (66 mL/min/kg), a moderate volume of distribution (1.6 L/kg), and a short half-life (t_1/2, 22 min) in rats.

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