GSK-1605786
- CAS No.
- 698394-73-9
- Chemical Name:
- GSK-1605786
- Synonyms
- CCX282-B;Vercirnon;GSK1605786;Traficet-EN;GSK-1605786;GSK 1605786;Vercirnon GSK1605786;Vercirnon, 10 mM in DMSO;4-(2-(4-tert-butylphenylsulfonamido)-5-chlorobenzoyl)pyridin-1(2H)-olate;4-(2-((4-(tert-Butyl)phenyl)sulfonamido)-5-chlorobenzoyl)pyridine 1-oxide
- CBNumber:
- CB42668435
- Molecular Formula:
- C22H21ClN2O4S
- Molecular Weight:
- 444.93
- MDL Number:
- MOL File:
- 698394-73-9.mol
- MSDS File:
- SDS
| Boiling point | 672.3±65.0 °C(Predicted) |
|---|---|
| Density | 1.29±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO: 25 mg/ml |
| form | A crystalline solid |
| pka | 7.07±0.10(Predicted) |
| color | White to off-white |
| FDA UNII | MWI54OUA12 |
GSK-1605786 price More Price(11)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 23131 | Vercirnon | 698394-73-9 | 1mg | $81 | 2024-03-01 | Buy |
| Cayman Chemical | 23131 | Vercirnon | 698394-73-9 | 5mg | $377 | 2024-03-01 | Buy |
| ChemScene | CS-4963 | Vercirnon 98.19% | 698394-73-9 | 5mg | $420 | 2021-12-16 | Buy |
| AK Scientific | 6855CR | Vercirnon | 698394-73-9 | 5mg | $517 | 2021-12-16 | Buy |
| ChemScene | CS-4963 | Vercirnon 98.19% | 698394-73-9 | 10mg | $600 | 2021-12-16 | Buy |
GSK-1605786 Chemical Properties,Uses,Production
Description
Vercirnon is an orally bioavailable antagonist of chemokine receptor 9 (CCR9) with an IC50 value of 5.4 nM for inhibition of CCL25-induced calcium mobilization in Molt-4 cells. It is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s = >10 μM for all). It also inhibits CCL25-induced Molt-4 chemotaxis in 0.1% BSA/HBSS and in 100% human AB serum (IC50s = 3.5 and 33.4 nM, respectively), as well as chemotaxis of human T cells stimulated by retinoic acid (RA) and mouse and rat thymocytes. Vercirnon binds allosterically to the intracellular side of CCR9 and prevents G protein coupling.
Uses
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].
in vivo
Vercirnon (GSK-1605786) (10、50 mg/kg；sc；每天两次；从 2 周龄开始至 12 周龄) 改善 TNFΔARE 小鼠模型中肠道炎症的严重程度[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. |
IC 50
CCR9: 10 nM (IC50)
References
[1] Walters MJ, 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. DOI:10.1124/jpet.110.169714
[2] Bekker P, et al. CCR9 Antagonists in the Treatment of Ulcerative Colitis. Mediators Inflamm. 2015;2015:628340. DOI:10.1155/2015/628340
[3] Zhang J, et al. Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3661-4. DOI:10.1016/j.bmcl.2015.06.046
GSK-1605786 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK-1605786 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29808 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7552 | 61 |
| MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4861 | 58 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Guangzhou QiYun Biotechnology Co., Ltd. | 020-61288194 61288195 | 505721671@qq.com | China | 3866 | 58 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71829 | 60 |
| Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 6188 | 55 |
