VX 702
Modify Date: 2024-01-05 11:31:01
VX 702 structure
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Common Name | VX 702 | ||
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| CAS Number | 745833-23-2 | Molecular Weight | 404.318 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 555.2±60.0 °C at 760 mmHg | |
| Molecular Formula | C19H12F4N4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 289.6±32.9 °C | |
Use of VX 702VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β.IC50 value: 4-20 nM [1]Target: p38α MAPKin vitro: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies [1]. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner [2]. 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]. |
| Name | vx-702 |
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| Synonym | More Synonyms |
| Description | VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β.IC50 value: 4-20 nM [1]Target: p38α MAPKin vitro: Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies [1]. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner [2]. 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]. |
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| Related Catalog | |
| References |
[2]. Braddock M, IDDB Meeting Report, 2005, March 14-15. |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 555.2±60.0 °C at 760 mmHg |
| Molecular Formula | C19H12F4N4O2 |
| Molecular Weight | 404.318 |
| Flash Point | 289.6±32.9 °C |
| Exact Mass | 404.089630 |
| PSA | 102.31000 |
| LogP | 0.76 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.629 |
| Storage condition | -20°C |
| 6-[Carbamoyl(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)nicotinamide |
| 3-Pyridinecarboxamide, 6-[(aminocarbonyl)(2,6-difluorophenyl)amino]-2-(2,4-difluorophenyl)- |
| VX702 |