Acumapimod

SKU: orb1299879

Description

Acumapimod (BCT-197) is an orally bioavailable small molecule that selectively inhibits p38α MAP kinase with an IC50 below 1 μM. It has been utilized in preclinical research to investigate p38α's role in inflammatory pathways, with studies demonstrating its activity in both cellular assays and animal models of inflammation.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 836683-15-9
• MW: 385.42
• Purity: 98.00% (May vary between batches)
• Formula: C₂₂H₁₉N₅O₂
• SMILES: Cc1ccc(cc1-n1ncc(C(=O)c2cccc(c2)C#N)c1N)C(=O)NC1CC1
• Target: p38 MAPK,Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.19 mM);DMSO:50 mg/mL (129.73 mM)

Bioactivity

• Target IC50:
  p38α:<1 μM
• In Vivo:
  Acumapimod increases survival and reduces the number of macrophages in bronchoalveolar lavage fluid (BALF) in a mouse model of infection with influenza H1N1 A/PR/8/34 when administered at a dose of 6 mg/kg
• Animal Research:
  In vivo, female BALB/c mice were infected intranasally with 150 pfu of influenza H1N1 A/Puerto Rico/8/34 and treated with Acumapimod(BCT197) (a closely related p38 MAPK inhibitor with an IC50 value of<1 μM, currently in clinical testing), dexamethasone or oseltamivir (Tamiflu) starting 24 h post infection. Body weight, bronchoalveolar lavage cells, cytokines, total protein and lactate dehydrogenase as well as serum cytokines were measured; a subset of animals was evaluated histopathologically.

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

Acumapimod, BCT 197, BCT197, BCT-197, Autophagy, inhibit, Inhibitor, p38, p38 MAPK, p38MAPK

Compound Identifiers

PubChem CID

11338127