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VX-702
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Product Name VX-702
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Catalog No.: CN00195
CAS No.: 745833-23-2
Molecular Formula: C19H12F4N4O2
Molecular Weight: 404.3 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Powder
Source:
Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
SMILES: Fc1ccc(c(c1)F)c1nc(ccc1C(=O)N)N(c1c(F)cccc1F)C(=O)N
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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].
Density1.5±0.1 g/cm3
Boiling Point555.2±60.0 °C at 760 mmHg
Flash Point289.6±32.9 °C
Exact Mass404.089630
PSA102.31000
LogP0.76
Vapour Pressure0.0±1.5 mmHg at 25°C
Storage condition-20°C