VU6000918 是毒蕈碱乙酰胆碱 (M4) 阳性变构调节剂，其对hM4 的EC50 值为 19 nM。
货号:ajcx38658
CAS:2101737-32-8
分子式:C18H17F2N5OS
分子量：389.42
溶解度:DMSO : 125 mg/mL (320.99 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].

VU6000918 demonstrates statistically significant AHL reversal (18%) from a low oral dose of 0.03 mg/kg and reaches maximal reversal (74%) from a 3 mg/kg dose, with a resulting in vivo plasma EC50 of 74 nM (0.66 nM unbound) based on terminal concentrations measured in the study animals (1.5 hr post-administration of 17j)[1].

[1]. James C Tarr, et al. Challenges in the development of an M 4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995.