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Product Details

VX-702 | P38alpha MAP kinase inhibitor

VX-702 (745833-23-2) is a  potent and selective inhibitor of p38 MAP kinases, p38α MAPK and p38β (KD = 3.7 and 17 nM respectively).1 Inhibits IL-6, IL-1β and TNFα production in LPS-primed blood.1 Inhibits p38 in platelets stimulated by thrombin, collagen, or thromboxane agonist U-46619 at 1 μM.2 Provides only modest clinical efficacy in rheumatoid arthritis.3,4 Delays platelet lesions and leads to better maintenance of stored platelets.5

References/Citations

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

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Catalog#  10-2181-0010

$40.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
745833-23-2
Catalog Number:
10-2181
Activity:
p38alpha MAP kinase inhibitor
Chemical Name:
6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide
Molecular Weight:
404.32
Molecular Formula:
C19H12F4N4O2
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 2 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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