Acumapimod( BCT-197 )

Catalog No. M16100 CAS No. 836683-15-9

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Product Name

Acumapimod
Note

Research use only, not for human use.
Brief 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).
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.
In Vitro

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

BCT-197
Pathway

MAPK/ERK Signaling
Target

p38 MAPK
Recptor

p38 MAPK
Research Area

Inflammation/Immunology
Indication

COPD

CAS Number

836683-15-9
Formula Weight

385.4185
Molecular Formula

C22H19N5O2
Purity

>98% (HPLC)
Solubility

DMSO: 10 mM
SMILES

O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2
Chemical Name

Benzamide, 3-[5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl]-N-cyclopropyl-4-methyl-

1. De Buck S, et al. CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700.

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