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VU0152100
本半岛bd体育手机客户端 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。
VU0152100图片
CAS NO: 409351-28-6
包装与价格：
包装 价格(元)
10mg 电议
50mg 电议

半岛bd体育手机客户端 介绍
VU0152100 是一种有效的、选择性的 M4 mAChR 变构增效剂，EC50 为 380 ± 93 nM。
Cas No. 409351-28-6
别名 3-氨基-N-[(4-甲氧基苯基)甲基]-4,6-二甲基噻吩并[2,3-B]吡啶-2-甲酰胺,VU152100
化学名 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Canonical SMILES CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)OC)N)C
分子式 C18H19N3O2S
分子量 341.43
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

VU0152100 is a selective and positive allosteric modulators of M4 receptor with the EC50 value of 380±93nM[1].

VU0152100 has shown a potent positive allosteric modulators that increase the response of the M4 receptor to the endogenous agonist ACh in in vitro study. In addition, VU0152100 has been reported to dese-dependently potentiate the response to the agonist (ACh) with the EC50 value of 1.9±0.2μM, and increase the maximal response to ACh to approximately 130%. Furthermore, VU0152100 has been revealed to enhance receptor activation by increasing the affinity of M4 for acetylcholine. Apart from these, VU0152100 has been found to induce a 20 to 25-fold leftward shift in the potency of ACh to displace [3H]NMS binding to M4 receptor with the Ki value from 252±19.7nM to 12.2±0.49nM [1].

References:
[1] Brady AE1, Jones CK, Bridges TM, Kennedy JP, Thompson AD, Heiman JU, Breininger ML, Gentry PR, Yin H, Jadhav SB, Shirey JK, Conn PJ, Lindsley CW. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53.
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