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

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

Cat. No.: HY-15724 Purity: 98.58%
Handling Instructions

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.

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 USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[3]

CCR9

10 nM (IC50)

In Vitro

Vercirnon (GSK-1605786) inhibits chemotaxis of primary CCR9-expressing cells to CCL25 with an IC50 of 6.8 nM. Vercirnon inhibits CCL25-Induced Chemotaxis of retinoic acid (RA)-Cultured Human T Cells. Vercirnon inhibits RA-cultured cell CCL25-medidated chemotaxis in 100% human AB serum resulted in an IC50 of 141 nM. Vercirnon is a potent inhibitor of CCL25-induced mouse and rat thymocyte chemotaxis with IC50 values of 6.9 nM and 1.3 nM, respectively[1].

In Vivo

Vercirnon (GSK-1605786) (10, 50 mg/kg; s.c.; twice per day; starting at 2 weeks of age until 12 weeks of age) ameliorates the severity of intestinal inflammation in the TNFΔARE mouse model[1].

Animal Model: C57BL/6 mice (TNFΔARE Mouse Model of Terminal Ileitis)[1]
Dosage: 10, 50 mg/kg
Administration: Subcutaneous; twice per day; starting at 2 weeks of age until 12 weeks of age
Result: Resulted in complete protection from the severe inflammation associated with TNF- overexpression at 50 mg/kg. A similar protective effect was also noted with a lower dose.
Clinical Trial
Molecular Weight

444.93

Formula

C₂₂H₂₁ClN₂O₄S

CAS No.

698394-73-9

SMILES

O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=CC=C(Cl)C=C2C(C3=CC=[N+]([O-])C=C3)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (56.19 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2475 mL 11.2377 mL 22.4754 mL
5 mM 0.4495 mL 2.2475 mL 4.4951 mL
10 mM 0.2248 mL 1.1238 mL 2.2475 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VercirnonGSK-1605786CCX282-BTraficet-ENGSK1605786GSK 1605786CCRCC chemokine receptororalbioavailableinflammatoryboweldiseasechemotaxischemokineInhibitorinhibitorinhibit

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Vercirnon
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HY-15724
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