GSK-1605786A
- Product Name
- GSK-1605786A
- CAS No.
- 886214-18-2
- Chemical Name
- GSK-1605786A
- Synonyms
- GSK1605786A;GSK 1605786A;GSK-1605786A;CCX282-Bsodium;Traficet-ENsodium;Vercirnon (sodiuM);GSK-1605786 sodium;LBRWQGMQARTQCO-UHFFFAOYSA-N
- CBNumber
- CB52668346
- Molecular Formula
- C22H20ClN2NaO4S
- Formula Weight
- 466.91297
- MOL File
- 886214-18-2.mol
GSK-1605786A Property
- form
- Solid
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- CS-0008549
- Product name
- Vercirnon(sodium)
- Purity
- 98.76%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- CS-0008549
- Product name
- Vercirnon(sodium)
- Purity
- 98.76%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-0008549
- Product name
- Vercirnon(sodium)
- Purity
- 98.76%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- CS-0008549
- Product name
- Vercirnon(sodium)
- Purity
- 98.76%
- Packaging
- 100mg
- Price
- $2520
- Updated
- 2021/12/16
GSK-1605786A Chemical Properties,Usage,Production
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. |
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
Raw materials
Preparation Products
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