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ML380
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ML380图片
CAS NO:1627138-52-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
ML380是一种有效的，亚型选择性和可透过血脑屏障的M5mAChR正变构调节剂(PAM)，对人和大鼠M5的EC50值分别为190和610nM。ML380对M1和M3mAChR亚型具有中等选择性。ML380可以增加Ach对M5mAChR的亲和力。
Cas No.1627138-52-6
Canonical SMILESO=C(C1CCN(S(=O)(C2=CC3=C(NN=C3)C=C2)=O)CC1)N(CC)CC4=CC=CC=C4C(F)(F)F
分子式C23H25F3N4O3S
分子量494.53
溶解度DMSO: 100 mg/mL (202.21 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s 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[1][2][3].

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[2].ML380 (0.01-30 μM) increases the ACh-stimulated IP accumulation and Ca2+ mobilization in CHO-hM5 cells[2].

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 (t1/2, 22 min) in rats[1].

[1]. Gentry PR, et, al. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). J Med Chem. 2014 Sep 25;57(18):7804-10. [2]. Berizzi AE, et, al. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol. 2016 Oct;90(4):427-36. [3]. Berizzi AE, et, al. Structure-Activity Relationships of Pan-Gα q/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. ACS Chem Neurosci. 2018 Jul 18;9(7):1818-1828.