1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR

Vercirnon (Synonyms: GSK-1605786; CCX282-B)

Cat. No.: HY-15724 Purity: 98.04%
Data Sheet SDS Handling Instructions

Vercirnon is a highly potent antagonist of CCR9, which has been implicated in the aetiology of inflammatory bowel diseases such as Crohn's disease.

For research use only. We do not sell to patients.
Vercirnon Chemical Structure

Vercirnon Chemical Structure

CAS No. : 698394-73-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $385 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

Vercirnon is a highly potent antagonist of CCR9, which has been implicated in the aetiology of inflammatory bowel diseases such as Crohn's disease. IC50 value: <7 nM (Molt-4 cells, CCR9 transfected cell, primary derived human T cells, and murine and rat thymocytes) Target: CCR9 in vitro: CCX282-B inhibits CCR9 mediated chemotaxis to CCL25 (IC50 <7 nM), measured in the Molt-4 cells, CCR9 transfected cell lines, primary derived human T cells, and murine and rat thymocytes.[1] CCX282-B inhibits CCR9-mediated Ca2+mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively.. CCX282-B inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. CCX282-B 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. [2] in vivo: CCX282-B also inhibits mouse and rat CCR9-mediated chemotaxis. Inhibition of CCR9 with CCX282-B results in normalization of Crohn's disease such as histopathology associated with the TNFΔARE mice. [2]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00540657 ChemoCentryx Celiac Disease October 2007 Phase 2
NCT00306215 ChemoCentryx Crohn's Disease March 2006 Phase 2
NCT00102921 ChemoCentryx Crohn Disease August 2004 Phase 2
NCT00540657 ChemoCentryx Celiac Disease October 2007 Phase 2
NCT00306215 ChemoCentryx Crohn's Disease March 2006 Phase 2
NCT00102921 ChemoCentryx Crohn Disease August 2004 Phase 2
NCT01318993 GlaxoSmithKline Crohn's Disease April 2011 Phase 3
NCT01536418 GlaxoSmithKline Crohn's Disease November 11, 2011 Phase 3
NCT01316939 GlaxoSmithKline Crohn's Disease May 2011 Phase 3
NCT01277666 GlaxoSmithKline Crohn's Disease December 2010 Phase 3
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References
M.Wt

444.93

Formula

C₂₂H₂₁ClN₂O₄S

CAS No.

698394-73-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Vercirnon
Cat. No.:
HY-15724
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