| Identification | Back Directory | [Name]
GSK-1605786 | [CAS]
698394-73-9 | [Synonyms]
CCX282-B
Vercirnon
GSK1605786
GSK-1605786
Traficet-EN
GSK 1605786
Vercirnon GSK1605786
4-(2-(4-tert-butylphenylsulfonamido)-5-chlorobenzoyl)pyridin-1(2H)-olate
Benzenesulfonamide, N-[4-chloro-2-[(1-oxido-4-pyridinyl)carbonyl]phenyl]-4-(1,1-dimethylethyl)-
chemotaxis,CCR,bioavailable,Vercirnon,oral,GSK 1605786,inhibit,inflammatory,Inhibitor,bowel,GSK1605786,chemokine,CC chemokine receptor,disease | [Molecular Formula]
C22H21ClN2O4S | [MOL File]
698394-73-9.mol | [Molecular Weight]
444.93 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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；每天兩次；從 2 周齡開始至 12 周齡) 改善 TNFΔARE 小鼠模型中腸道炎癥的嚴(yán)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.
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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 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|