Molecular Weight(MW): 404.3
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
Cited by 6 Publications
2 Customer Reviews
Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: *p < 0.05, ***p < 0.001.
Mol Immunol 2014 62(2), 266-76. VX-702 purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.|
|Features||Highly selective, orally active inhibitor of p38 MAPK.|
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.  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. 
|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.  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.  VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.|
|In vitro||DMSO||81 mg/mL (200.34 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
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