Network Version
VX-702 Data Sheet
| Product Name: | VX-702 |
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|---|---|---|
| CAS No.: | 745833-23-2 | |
| Cat. No.: | HY-10401 | |
| MWt: | 404.32 | |
| Formula: | C19H12F4N4O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 42 mg/mL | |
| Mechanisms: | Target: Inflammation/Immunology | |
| Biological Activity: | ||
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VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β[1].
IC50 & Target: p38α MAPK[1]
In Vitro: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies[1]. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner[2]. In Vivo: The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally[2]. VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score[3]. |
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