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| | VX 702 Chemical Properties |
| Boiling point | 555.2±60.0 °C(Predicted) | | density | 1.503 | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 2 mg/ml) | | pka | 10.65±0.50(Predicted) | | form | solid | | color | White | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | CAS DataBase Reference | 745833-23-2 |
| | VX 702 Usage And Synthesis |
| Biological activity | VX-702 is a highly selective p38α MAPK inhibitor, 14-fold more potent against p38α than against p38β. Phase 2. | | Description | VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis. | | Uses | VX-702 is a p38 mitogen-activated protein kinase (MAPK) inhibitor. VX-702 had no effect on platelet aggregation induced by any of the p38 MAPK agonists. VX-702 has potential use in the treatment of inflammation, rheumatoid arthritis and cardiovascular diseases. | | Uses | VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion. It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively. VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.[Cayman Chemical] | | Definition | ChEBI: 6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)-3-pyridinecarboxamide is a phenylpyridine. | | storage | +4°C | | References | 1) Goldstein?et al.?(2010),?Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders; J. Med. Chem.,?53?2345
2) Kuliopulos?et al.?(2004),?Effect of selective inhibition of the p38 MAP kinase pathway on platelet aggregation; Thromb. Haemostasis,?92?1387
3) Damianov?et al.?(2009),?Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies; Arthrit. Rheumat.,?60?1232
4) Ding?et al. (2006),?Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome; Curr. Opin. Investig. Drugs,?7?1020
5) Scripchenko?et al.?(2013),?An inhibition of p38 mitogen activated protein kinase delays the platelet storage lesion; PLoS One,?8(8)e?70732 |
| | VX 702 Preparation Products And Raw materials |
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