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VU 0357121
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。
VU 0357121图片
CAS NO:433967-28-3
包装与价格:
包装价格(元)
10mg电议
25mg电议

产品介绍
VU 0357121 是一种正向且高度选择性的 mGlu5R 别构调节剂 (PAM),EC50 为 33 nM。
Cas No.433967-28-3
化学名4-butoxy-N-(2,4-difluorophenyl)benzamide
Canonical SMILESCCCCOC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)F
分子式C17H17F2NO2
分子量305.32
溶解度DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 15 mg/ml
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

VU0357121 is a novel positive and highly selective allosteric modulator (PAM) of mGlu5R with EC50 of 33 nM.IC50 Value: 33 nM(EC50)Target: mGluR5in vitro: VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. in vivo:

References:
[1]. Hammond, Alexis S.; Rodriguez, Alice L.; Townsend, Steven D. et al. Discovery of a Novel Chemical Class of mGlu5 Allosteric Ligands with Distinct Modes of Pharmacology. ACS Chemical Neuroscience (2010), 1(10), 702-716.