Description
VX-702 can inhibit p38 mitogen-activated protein kinase with IC50 of 4-20 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C19H12F4N4O2
Chemical Name
1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea
Solubility
DSMO 81 mg/mL Water
In vitro
As a second generation p38 MAPK inhibitor, VX-702 can inhibit p38 mitogen-activated protein kinase with IC50 of 4-20 nM.Pre-treatment of platelets with 1 microM VX-702 completely inhibited activation of p38 MAPK by thrombin, SFLLRN, AYPGKF, U46619, and collagen.There was no effect of VX-702 on platelet aggregation induced by any of the agonists in the presence or absence of aspirin, heparin or apyrase. VX-702 has no effect on collagen-mediated platelet aggregation. VX-702 do not significantly affect platelet function and would not be expected to contribute to an elevated risk of bleeding side-effects in treated patients. VX-702 shows potential treatment of inflammation, rheumatoid arthritis and cardiovascular diseases.
In vivo
VX-702 is not a substrate for renal organic anion and organic cation transport systems. In rat kidney (IPRK) model, VX-702 excretion was linear over the range of 100ng/mL to 600 ng/mL.
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