GSK-1605786A manufacturers
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| | GSK-1605786A Basic information |
| Product Name: | GSK-1605786A | | Synonyms: | GSK 1605786A;GSK1605786A;GSK-1605786A;Vercirnon (sodiuM);LBRWQGMQARTQCO-UHFFFAOYSA-N;CCX282-Bsodium;GSK-1605786 sodium;Traficet-ENsodium | | CAS: | 886214-18-2 | | MF: | C22H20ClN2NaO4S | | MW: | 466.91297 | | EINECS: | | | Product Categories: | | | Mol File: | 886214-18-2.mol |  |
| | GSK-1605786A Chemical Properties |
| form | Solid | | color | Light yellow to yellow |
| | GSK-1605786A Usage And Synthesis |
| Uses | Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon sodium 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 (GSK1605786A) sodium (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.
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| | 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-1605786A Preparation Products And Raw materials |
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