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VX-702

Cat. No. M2317
VX-702 Structure
Size Price Availability Quantity
25mg USD 87  USD87 In stock
50mg USD 165  USD165 In stock
100mg USD 297  USD297 In stock
200mg USD 537  USD537 In stock
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Quality Control & Documentation
Biological Activity

VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM. In an ex vivo blood assay primed with LPS, VX-702 dose-dependently inhibited the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/ml, respectively). This activation was completely or partially inhibited by pre-incubation with 1 μM of VX-702 (IC50 = 4 to 20 nM). VX-702 had no effect on platelet aggregation induced by any of the p38 MAPK agonists.

Chemical Information
Molecular Weight 404.3
Formula C19H12F4N4O2
CAS Number 745833-23-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Andrey Skripchenko, et al. P38 mitogen activated protein kinase inhibitor improves platelet in vitro parameters and in vivo survival in a SCID mouse model of transfusion for platelets stored at cold or temperature cycled conditions for 14 days

[2] S J Wagner, et al. Amelioration of lesions associated with 24-hour suboptimal platelet storage at 16 °C by a p38MAPK inhibitor, VX-702

[3] Mitalee Tamhane, et al. Comparative renal excretion of VX-702, a novel p38 MAPK inhibitor, and methotrexate in the perfused rat kidney model

[4] Nemanja Damjanov, et al. 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

[5] Changhai Ding. Drug evaluation: VX-702, a MAP kinase inhibitor for rheumatoid arthritis and acute coronary syndrome

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  Catalog
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Keywords: VX-702 supplier, p38 MAPK, inhibitors, activators


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