VX-702

SKU: orb1305373

Description

VX-702 is an investigational oral small molecule with high specificity for p38α MAPK, showing 14-fold selectivity over p38β. It has been studied in clinical trials for rheumatoid arthritis and is used in research to investigate p38α signaling in inflammatory disease models, both in vitro and in vivo.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 745833-23-2
• MW: 404.32
• Purity: 99.19%
• Formula: C₁₉H₁₂F₄N₄O₂
• SMILES: NC(=O)N(c1ccc(C(N)=O)c(n1)-c1ccc(F)cc1F)c1c(F)cccc1F
• Target: Autophagy,p38 MAPK
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.95 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:60 mg/mL (148.4 mM)

Bioactivity

• Target IC50:
  p38α:4 nM-20 nM
• In Vivo:
  VX-702 does not inhibit platelet aggregation induced by p38 MAPK activators. Treatment with VX-702 (1 μM) can completely or partially suppress p38 activity induced by various platelet activators, including thrombin, AYPGKF, SFLLRN, U46619, and collagen, with an IC50 ranging from 4-20 nM. Additionally, VX-702 dose-dependently inhibits the production of IL-6 (IC50: 59 ng/ml), IL-1β (IC50: 122 ng/ml), and TNFα (IC50: 99 ng/ml).
• In Vitro:
  Administering VX-702 (0.1 mg/kg) twice daily exhibited effects similar to those of methotrexate (0.1 mg/kg). Furthermore, the efficacy of administering VX-702 (5 mg/kg) twice daily was akin to that of a once-daily dose of prednisolone (10 mg/kg). The MI/AAR ratio in the group treated with VX-702 (50 mg/kg) was significantly lower compared to both the control group and the group treated with VX-702 at 5 mg/kg. VX-702 has a half-life of 16-20 hours, a clearance volume of 3.75 L, and a distribution volume of 73 L/kg. It selectively inhibits the activity of p38 MAPK without affecting ERKs and JNKs.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

VX 702, VX702, VX-702, Inhibitor, inhibit, p38 MAPK, p38α, p38MAPK, Autophagy, 479543-46-9

Compound Identifiers

PubChem CID

10341154