VU 0357121

A positive allosteric modulator of mGluR5

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库存: 现货

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10mg

￥687.00

550.00

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25mg

￥1437.00

1150.00

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货号: ajci20416
CAS: 433967-28-3
别名:
分子式: C17H17F2NO2
分子量: 305.32
纯度: >98%
溶解度: DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 15 mg/ml
储存: Store at -20°C
库存: 现货

Background

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:

参考文献:
[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.