Acumapimod

SKU: orb1223909

Description

An orally active, potent p38 MAPK inhibitor that potently inhibits ex vivo LPS‐induced TNFα secretion with an IC50 of 44 ng/mL (115 nM); inhibits LPS‐stimulated TNFα release in the human whole blood assay with IC50 of 24 nM; shows antiinflammatory activity for treatment of acute as opposed to chronic inflammation disorders.COPD Phase 1 Clinical.

Key Properties

• CAS Number: 836683-15-9
• MW: 385.4185
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₉N₅O₂
• SMILES: O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2
• Target: p38 MAPK
• Solubility: DMSO: 10 mM

Bioactivity

• In Vivo:
  Acumapimod is an oral low-molecular-weight p38 inhibitor currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of Acumapimod (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients.
• In Vitro:
  Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM.

Storage & Handling

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

Alternative Names

BCT-197

Quick Database Links

Gene Symbol

p38 MAPK