2​ Biological Activity The activation of p38 MAPKs leads to gene transcription and translation, followed by an increase in production of inflammatory mediators, such as TNFα, IL-1β, cyclooxygenase (COX)-2, IL-6, IL-12 and IFNγ, [2] all of which have been demonstrated to play important roles in autoimmune diseases such as rheumatoid arthritis (RA) and/or cardiovascular diseases. In an ex vivo blood assay primed with LPS, VX-702 dose-dependently inhibited the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/ml, respectively). [3] To determine the effects, if any, of VX-702 on platelet function alone, or in conjunction with other commonly used anti-platelet therapies, gel-filtered platelets were prepared from healthy individuals (n = 6) for an ex vivo study. [4], [5] This activation was completely or partially inhibited by pre-incubation with 1 μM of VX-702 (IC50 = 4 to 20 nM). VX-702 had no effect on platelet aggregation induced by any of the p38MAPK agonist. 3​ References: [1] Ding C. et al. Curr Opin Investig Drugs. 2006 Nov;7(11):1020-5 [2] Kuliopulos A et al. Thromb Haemost. 2004 Dec;92(6):1387-93 The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.