COA | MSDS | HPLC | NMR |
CAS No: | 433967-28-3 |
Molecular formula(MF) | C17H17F2NO2 |
Molecular Weight(MW): | 305.32 |
Alias |
In vitro | DMSO | 61 mg/mL (199.79 mM) |
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Ethanol | 21 mg/mL (68.78 mM) | |
Water | <1 mg/mL |
Description | VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes. | ||
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Targets |
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In 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. [1] VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. [2] |