Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It effectively inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells, exhibiting IC50 values of 5.4 nM and 3.4 nM, respectively. Demonstrating high selectivity, Vercirnon sodium does not significantly affect CCR1-12 or CX3CR1-7, with IC50 values exceeding 10 µM for these receptors. Additionally, it inhibits CCL25-directed chemotaxis equally well in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 5 days | $ 347.00 | |
10 mg | 5 days | $ 541.00 | |
1 mL * 10 mM (in DMSO) | 5 days | $ 356.00 |
Description | Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent CCR9 antagonist. It effectively inhibits CCR9-mediated calcium mobilization and chemotaxis in Molt-4 cells, exhibiting IC50 values of 5.4 nM and 3.4 nM, respectively. Demonstrating high selectivity, Vercirnon sodium does not significantly affect CCR1-12 or CX3CR1-7, with IC50 values exceeding 10 µM for these receptors. Additionally, it inhibits CCL25-directed chemotaxis equally well in both CCR9 splice variants, CCR9A and CCR9B, with IC50 values of 2.8 nM and 2.6 nM, respectively. |
Targets&IC50 | CCR9:10 nM (IC50) |
In vitro | Vercirnon (GSK-1605786) sodium effectively suppresses the movement of primary cells expressing CCR9 towards CCL25, demonstrating an inhibition concentration (IC 50) of 6.8 nM. It also significantly blocks the CCL25-induced migration of retinoic acid (RA)-cultured human T cells. In the presence of 100% human AB serum, Vercirnon sodium impedes the chemotaxis mediated by CCL25 in RA-cultured cells, achieving an IC 50 of 141 nM. Moreover, it is a highly efficient inhibitor against the migration of mouse and rat thymocytes triggered by CCL25, with IC 50 values of 6.9 nM and 1.3 nM, respectively[1]. |
In vivo | Vercirnon (GSK1605786A) sodium administered subcutaneously at doses of 10 and 50 mg/kg, twice per day from 2 to 12 weeks of age, effectively reduces the severity of intestinal inflammation in the TNFΔARE mouse model (C57BL/6 mice with terminal ileitis)[1]. At a dose of 50 mg/kg, it resulted in complete protection against severe inflammation caused by TNF- overexpression, with a similar protective effect observed at the lower dose. |
Synonyms | GSK-1605786 sodium, CCX282-Bsodium, Traficet-ENsodium |
Molecular Weight | 467.92 |
Formula | C22H21ClN2NaO4S |
CAS No. | 886214-18-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Vercirnon sodium 886214-18-2 GSK-1605786 sodium CCX282-Bsodium Traficet-ENsodium inhibitor inhibit