您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > VU6000918
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
VU6000918
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。
VU6000918图片
CAS NO:2101737-32-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
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。
Cas No.2101737-32-8
分子式C18H17F2N5OS
分子量389.42
溶解度DMSO : 125 mg/mL (320.99 mM; Need ultrasonic)
储存条件Store at -20°C
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

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.