VU0424465

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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 K_i value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.

For research use only. We do not sell to patients.

VU0424465 Chemical Structure

CAS No. : 1428630-85-6

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

mGlu₅

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]

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].

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

Molecular Weight

326.36

Formula

C₁₉H₁₉FN₂O₂

CAS No.

1428630-85-6

SMILES

O=C(N[C@H](C)C(O)(C)C)C1=NC=C(C=C1)C#CC2=CC=CC(F)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Sengmany K, et al. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. 2017;115:60-72. [Content Brief]

[2]. Rook JM, Noetzel MJ, Pouliot WA, et al. Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol Psychiatry. 2013;73(6):501-509. [Content Brief]

VU0424465 Related Classifications

Neurological Disease

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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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