VU0424465

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].

Product Specifications

CAS Number

[1428630-85-6]

Product Name Alternative

Monobromobimane,2-Ethyl-3,5-dimethylpyrazine-13C11

UNSPSC

12352005

Target

MGluR; PERK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vu0424465.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C19H19FN2O2

Molecular Weight

326.36

References & Citations

[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.|[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.