VU0424465

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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。

CAS NO:

1428630-85-6

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，K_i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 K_ivalue 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.