ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR , with EC 50 s of 190 and 610 nM for human and rat M5 , respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR In Vitro ML380 (0.01 nM-100 μM) robustly stimulates inositol phosphate (IP) accumulation and Ca 2+ mobilization in CHO-hM 5 cells, with pEC 50 s of 5.33 and 5.71, respectively. ML380 (0.01-30 μM) increases the ACh-stimulated IP accumulation and Ca 2+ mobilization in CHO-hM 5 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 190 nM (hM5), 610 nM (rM5)
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ML380
CAS number：1627138-52-6 molecular formula：C23H25F3N4O3S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1627138-52-6 | molecular formula | C23H25F3N4O3S |
| molecular weight | 494.53 g/mol | Exact mass | ≥99% |
| PSA | 94.800 Ų | logp | 3.400 |
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