Vercirnon (sodium)

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all) . Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively[1].

Product Specifications

CAS Number

[886214-18-2]

Product Name Alternative

GSK-1605786 (sodium) ; CCX282-B (sodium) ; Traficet-EN (sodium)

UNSPSC

12352005

Target

CCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/vercirnon-sodium.html

Concentration

10mM

Purity

98.04

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=C(C(C)(C)C)C=C1)([N-]C2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O.[Na+]

Molecular Formula

C22H20ClN2NaO4S

Molecular Weight

466.91

References & Citations

[1]Walters MJ, et al. Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther. 2010 Oct;335 (1) :61-9.|[2]Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340.|[3]Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25 (17) :3661-4.