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编 号:F160501
分子式:C19H19FN2O2
分子量:326.36
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生物活性:
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.

体外研究:
VU0424465 exhibits robust agonist activity and induces calcium mobilization in the absence of glutamate (EC50 = 171 ± 15 nM, maximum efficacy 65% compared to glutamate).VU0424465 potentiates glutamate-induced calcium mobilization, with EC50 of 1.5 ± 0.8 nM.VU0424465 shows significant bias away from iCa2+ mobilization and toward IP1 accumulation (110-fold) and ERK1/2 phosphorylation (9-fold) in HEK293A-mGlu5-low cells.
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