Acumapimod

Names

[ Name ]:
Acumapimod

[Synonym ]:
Benzamide, 3-[5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl]-N-cyclopropyl-4-methyl-
3-[5-Amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide
acumapimod

Biological Activity

[Description]:

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK

Research Areas >> Inflammation/Immunology

[Target]

IC50: less than 1 μM (p38α)[1]

[In Vitro]

Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM.

[In Vivo]

BCT197 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 BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients[2].

[References]

[1]. Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.

[2]. De Buck S, et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197. CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700.

[Related Small Molecules]

SB203580 | SB202190 (FHPI) | Doramapimod (BIRB 796) | LY2228820 | SB 239063 | Losmapimod | PD 169316 | Talmapimod | Tat-NR2B9c | Dehydrocorydaline chloride | TAK-715 | VX 702 | VX-745 | SKF 86002 | PH-797804

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
675.6±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₂H₁₉N₅O₂

[ Molecular Weight ]:
385.419

[ Flash Point ]:
362.4±31.5 °C

[ Exact Mass ]:
385.153870

[ LogP ]:
2.57

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.708

[ Storage condition ]:
2-8℃

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.