Bulk Inquiry
Vercirnon
- GSK-1605786 - CCX282-B - Traficet-EN
- Soluble in DMSO
- MF: C22H21ClN2O4S
- MW: 444.93
Description
Vercirnon (GSK-1605786; CCX282-B) is an orally available antagonist that selectively targets the Chemokine Receptor 9 (CCR9), with IC50 values of 5.4 nM and 3.4 nM for CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells, respectively. Biologically, it functions by binding to the intracellular side of the receptor to act as an allosteric antagonist, preventing G-protein coupling and inhibiting the migration of inflammatory T-cells to the intestines.
Vercirnon blocks CCL25-mediated lymphocyte trafficking to the small intestine. It is used to research chemokine signaling, GPCR allostery, and immune-cell migration. Additionally, it has been studied as a way to modulate gut-homing leukocytes in Crohn's disease and inflammatory bowel disease.
Key Features
- Potent and selective CCR9 antagonist
- IC50: 5.4 nM for calcium mobilization
- IC50: 3.4 nM for CCR9-mediated chemotaxis
- Binds an intracellular allosteric GPCR pocket
- Prevents CCR9 coupling to G proteins
Applications
- CCR9–CCL25 signaling research
- Chemokine receptor antagonist screening
- Lymphocyte chemotaxis and gut-homing studies
- Inflammatory bowel disease and Crohn’s disease models
- Intracellular GPCR and allosteric research
More Information
| Parent CAS No. | 698394-73-9 |
|---|---|
| Chemical Name | 4-(2-(4-Tert-butylphenylsulfonamido)-5-chlorobenzoyl)pyridine 1-oxide |
| SMILES | C1C(Cl)=CC(C(C2C=C[N+]([O-])=CC=2)=O)=C(NS(C2C=CC(C(C)(C)C)=CC=2)(=O)=O)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C22H21ClN2O4S/c1-22(2,3)16-4-7-18(8-5-16)30(28,29)24-20-9-6-17(23)14-19(20)21(26)15-10-12-25(27)13-11-15/h4-14,24H,1-3H3 |
| InChiKey | JRWROCIMSDXGOZ-UHFFFAOYSA-N |
| CID | 10343454 |
| Short Description | CCR9 antagonist |
References
- MJ Walters 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.
- B Eksteen et al. GSK-1605786, a selective small-molecule antagonist of the CCR9 chemokine receptor for the treatment of Crohn's disease. IDrugs. 2010 Jul;13(7):472-81.
- C Oswald et al. Intracellular allosteric antagonism of the CCR9 receptor. Nature. 2016 Dec 15;540(7633):462-465.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1179 | A1B1 hydrochloride |
From $137.50 |
| 1559 | SB 265610 |
From $132.00 |
| 1620 | WZ 811 |
From $88.00 |
| 1738 | AMD 3100 |
From $99.00 |
| 1800 | CXCR3 Antagonist 6c |
From $148.50 |
| 1930 | AMD 3465 hexahydrobromide |
From $93.50 |
| 2082 | BX 471 |
From $115.50 |
| 2255 | AZD8797 |
From $132.00 |
| 2593 | SB 332235 |
From $115.50 |
| 2636 | YJC-10592 |
From $159.50 |
| 2665 | Cenicriviroc |
From $176.00 |
| 2842 | AZD2098 |
From $137.50 |
| 2861 | ZK 756326 dihydrochloride |
From $99.00 |
| 2921 | LIT-927 |
From $104.50 |
| 2993 | UNBS5162 |
From $104.50 |
| 3774 | LN6023 dihydrochloride |
From $165.00 |
