2. Neuronal Signaling GPCR/G Protein Cell Cycle/DNA Damage
  3. mGluR PERK
  4. VU0424465

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。

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VU0424465 Chemical Structure

VU0424465 Chemical Structure

CAS No. : 1428630-85-6

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VU0424465 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2].

IC50 & Target

mGlu5

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
4.9 nM
Compound: 19, VU0424465, ML273
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
[PMID: 24050755]
HEK293 EC50
904 nM
Compound: 19, VU0424465, ML273
Agonist activity at rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
Agonist activity at rat mGluR5 stably expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo-4AM dye-based fluorescence assay
[PMID: 24050755]
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 EC50 of 1.5 ± 0.8 nM[2].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

VU0424465 相关抗体:
分子量

326.36

Formula

C19H19FN2O2
CAS 号
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.
纯度 & 产品资料
参考文献

VU0424465 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU04244651428630-85-6VU 0424465VU-0424465mGluRPERKMetabotropic glutamate receptorsProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasebiased agonismmetabotropic glutamate receptor 5positive allosteric modulatorHEK cellscortical neuronsInhibitorinhibitorinhibit

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