A457

A457 is a prokineticin receptor PKR2 antagonist, with an IC50 of 102 nM. A457 can rescue the cell surface expression and function of P290S PKR2, but not W178S and G234D PKR2[1].

Product Specifications

CAS Number

[1233923-95-9]

UNSPSC

12352005

Target

Prokineticin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Others

Assay Protocol

https://www.medchemexpress.com/a457.html

Smiles

O=C(N(CC(C)C)CC1=CC(Cl)=C2OCCCOC2=C1)C3CN(CC3)CC4=CC=CC=C4

Molecular Formula

C26H33ClN2O3

Molecular Weight

457.00

References & Citations

[1]Dan-Na Chen, et al. Functional rescue of Kallmann syndrome-associated prokineticin receptor 2 (PKR2) mutants deficient in trafficking. J Biol Chem. 2014 May 30;289 (22) :15518-26.