| Identification | Back Directory | [Name]
VX 702 | [CAS]
745833-23-2 | [Synonyms]
VX 702
CS-1840
VX702;VX-702
VX 702 USP/EP/BP
(479543-46-9) vx 702
2-(2,4-Difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide
6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide
3-Pyridinecarboxamide, 6-[(aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-
6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide VX-702
VX 702 6-[(Aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)-3-pyridinecarboxamide | [Molecular Formula]
C19H12F4N4O2 | [MDL Number]
MFCD11616590 | [MOL File]
745833-23-2.mol | [Molecular Weight]
404.318 |
| Chemical Properties | Back Directory | [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) | [form ]
solid | [pka]
10.65±0.50(Predicted) | [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 |
| Hazard Information | Back Directory | [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.1 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.1 VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.2 Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.3 | [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. | [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[2].
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[3]. | [storage]
Store at -20°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 |
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| Company Name: |
J & K SCIENTIFIC LTD.
|
| Telephone: |
18210857532 18210857532 |
| Website: |
https://www.jkchemical.com |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|