产品
编 号:F357410
分子式:C17H17F2NO2
分子量:305.32
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.

体外研究:
VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.
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