VU 0357121 是一种高选择性的mGlu5R正变构调节剂 ，EC50为 33 nM。

VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes.

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. [1] VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. [2]

433967-28-3

C17H17F2NO2

305.325

Ethanol:30.5 mg/mL (100 mM)
DMSO:30.5 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years