Acumapimod (BCT-197)

• CAT Number: I001154
• CAS Number: 836683-15-9
• Molecular Formula: C22H19N5O2
• Molecular Weight: 385.42
• Purity: 98%
• Synonyms: BCT-197; BCT197; BCT 197; BCT197A2201; Acumapimod;3-(5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl)-N-cyclopropyl-4-methylbenzamide
• Target: Autophagy
• Solubility: Soluble in DMSO, not in water
• Appearance: Yellow to orange solid powder
• Storage: Store at -20°C
• IUPAC Name: 3-[5-amino-4-(3-cyanobenzoyl)pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide
• InChI: InChI=1S/C22H19N5O2/c1-13-5-6-16(22(29)26-17-7-8-17)10-19(13)27-21(24)18(12-25-27)20(28)15-4-2-3-14(9-15)11-23/h2-6,9-10,12,17H,7-8,24H2,1H3,(H,26,29)
• InChIKey: VGUSQKZDZHAAEE-UHFFFAOYSA-N
• SMILES: O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2

Acumapimod（Cat No.:I001154）, also referred to as BCT-197, is a powerful inhibitor of p38 mitogen-activated protein kinase (MAPK). It specifically targets p38α and p38β, two isoforms of the p38 protein kinases. These kinases play a crucial role in regulating the production of various inflammatory mediators. By inhibiting p38 MAPK, acumapimod helps suppress the inflammatory response, making it a potential therapeutic agent for inflammatory conditions and diseases. Its ability to modulate p38 signaling pathways makes it a valuable tool in studying the role of p38 MAPK in inflammation and developing targeted therapies.

Reference

1. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. doi:
10.1517/13543784.2015.1006358. Epub 2015 Jan 20.

Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary
disease.

Norman P(1).

Author information:
(1)Norman Consulting , 18 Pink Lane, Burnham, Bucks, SL1 8JW , UK
.

INTRODUCTION: The p38 protein kinases, in particular p38α and p38β, regulate the
production of multiple inflammatory mediators. Consequentially, considerable
effort has been focused on trying to develop p38 inhibitors for the treatment of
inflammatory diseases. Some 20 p38 inhibitors have progressed to clinical
development, mostly for the treatment of rheumatoid arthritis, but with little
success. Increasingly, interest has turned to their use in other indications and
notably chronic obstructive pulmonary disease (COPD).
AREAS COVERED: In this review, the author discusses the eight p38 inhibitors that
have been clinically evaluated. Acumapimod is the only one of four orally
delivered inhibitors that remains in active development while Phase II results of
PH-797804 and losmapimod are compared. The activity of two inhibitors designed
for inhaled delivery, RV-568 and PF-03715455, is compared but little is known
about AZD-7624 or the discontinued GSK-610677.
EXPERT OPINION: Results from animal models provide a clear rationale for
developing p38 inhibitors for COPD, and appear to be (partially) validated by the
efficacy seen with PH-797804 and losmapimod. Inhaled delivery provides the
opportunity to enhance p38 inhibition in the lung while reducing unwanted
systemic effects of p38 inhibition. Validation of this hypothesis should come
from the results of the recently completed Phase II study with RV-568.