R1487 (Hydrochloride)

SKU: orb1220500

Description

R1487 (Hydrochloride) is an orally bioavailable and highly selective inhibitors of p38α.

Key Properties

• CAS Number: 449808-64-4
• MW: 424.83
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₉ClF₂N₄O₃
• SMILES: Cl.Cn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
• Target: p38 MAPK
• Solubility: DMSO:20.83 mg/mL (49.03 mM)

Bioactivity

• In Vivo:
  R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β. Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively.
• In Vitro:
  R1487 Hydrochloride exhibits IC50 values of 10 nM for p38α inhibition and 200 nM for the inhibition of TNFα induced production of IL-1β. R1487 (Compounds 2a) inhibits production of TNFα by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

p38 MAPK