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VU0424465
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
VU0424465图片
CAS NO:1428630-85-6
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
VU0424465 是一种正向变构调节-激动剂，用于mGlu5介导的iCa2+动员。VU0424465 在 MPEP 变构结合位点表现出高亲和力，Ki值为11.8 nM。VU0424465 也是皮质神经元中pERK1/2的激动剂。
生物活性

VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist formGlu5mediated iCa2+mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Kivalue of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons[1][2].

IC50& Target

mGlu5

 

体外研究
(In Vitro)

VU0424465 exhibits robust agonist activity and induces calcium mobilization in the absence of glutamate (EC50= 171 ± 15 nM, maximum efficacy 65% compared to glutamate)[2].
VU0424465 potentiates glutamate-induced calcium mobilization, with EC50of 1.5 ± 0.8 nM[2].
VU0424465 shows significant bias away from iCa2+mobilization and toward IP1accumulation (110-fold) and ERK1/2 phosphorylation (9-fold) in HEK293A-mGlu5-low cells[1].

分子量

326.36

Formula

C19H19FN2O2

CAS 号

1428630-85-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.