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

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

Cat. No.: HY-15724 Purity: 98.19%
COA 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
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 462 In-stock
Solid
5 mg USD 330 In-stock
10 mg USD 520 In-stock
25 mg USD 1050 In-stock
50 mg USD 1650 In-stock
100 mg USD 2450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Vercirnon:

Vercirnon Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Vercirnon

View All CCR Isoform Specific Products:

View All Isoforms
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Vercirnon Related Antibodies
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C22H21ClN2O4S
CAS No.
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)

*"≥" 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 available by MCE.
Purity & Documentation
References
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Vercirnon Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Vercirnon698394-73-9GSK-1605786 CCX282-B Traficet-ENGSK1605786GSK 1605786CCRCC chemokine receptororalbioavailableinflammatoryboweldiseasechemotaxischemokineInhibitorinhibitorinhibit

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