IC50: 13 nM BMS-582949 is a p38 MAPK inhibitor p38R MAP kinase plays a key role in regulating the biosynthesis of various inflammatory cytokines, such as tumor necrosis factor alpha and interleukin-1β. Thus, p38R inhibitors are considered as a promising therapy for inflammatory disease treatment. In vitro: BMS-582949 was found to be 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective against Raf. Moreover, the binding mode of BMS-582949 with p38R was further demonstrated by X-ray crystallographic analyses . In vivo: In a pseudoestablished rat adjuvant arthritis model, BMS-582949 at doses of 10 and 100 mg/kg was found to display dose-dependent reduction in paw swelling with qd dosing. In addition, with bid dosing at doses of 1 and 5 mg/kg, BMS-582949 showed improved efficacy, resulting in great reduction in paw swelling. Moreover, the statistically significant reduction in paw swelling was also observed with the treatment of BMS-582949 at doses as low as 0.3 mg/kg bid . Clinical trial: A multicenter FDG-PET trial showed that in stable atherosclerosis, 12 weeks of treatment with BMS-582949 was not able to reduce arterial inflammation or hs-CRP when compared with placebo, while intensification of statin therapy could decrease arterial inflammation significantly .

Product information

CAS Number: 623152-17-0

Molecular Weight: 406.48

Formula: C22H26N6O2

Chemical Name: 4-{[5-(cyclopropylcarbamoyl)-2-methylphenyl]amino}-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide

Smiles: CCCNC(=O)C1=CN2N=CN=C(NC3=CC(=CC=C3C)C(=O)NC3CC3)C2=C1C

InChiKey: GDTQLZHHDRRBEB-UHFFFAOYSA-N

InChi: InChI=1S/C22H26N6O2/c1-4-9-23-22(30)17-11-28-19(14(17)3)20(24-12-25-28)27-18-10-15(6-5-13(18)2)21(29)26-16-7-8-16/h5-6,10-12,16H,4,7-9H2,1-3H3,(H,23,30)(H,26,29)(H,24,25,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.