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Vercirnon

Cat. No. M13929

All AbMole products are for research use only, cannot be used for human consumption.

Vercirnon Structure
Synonym:

GSK-1605786; CCX282-B; Traficet-EN

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Quality Control & Documentation
Biological Activity

Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon 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.

Chemical Information
Molecular Weight 444.93
Formula C22H21ClN2O4S
CAS Number 698394-73-9
Solubility (25°C) DMSO ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Rei Morikawa, et al. Role of CC chemokine receptor 9 in the progression of murine and human non-alcoholic steatohepatitis

[2] Lynda J Haberer, et al. Single-Dose Pharmacokinetics of the CCR9 Receptor Antagonist Vercirnon in Healthy US and Japanese Subjects

[3] Mark Lwenberg, et al. Next-Generation Therapeutics for IBD

[4] Lynda J Haberer, et al. Effects of vercirnon on the activity of CYP3A4, CYP2C19 and CYP2C8 enzymes and BCRP and OATP1B1 transporters using probe substrates

[5] Kristen O Arseneau, et al. Vercirnon for the treatment of Crohn's disease

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  Catalog
Abmole Inhibitor Catalog




Keywords: Vercirnon, GSK-1605786; CCX282-B; Traficet-EN supplier, CCR, inhibitors, activators

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