BMS-582949 - 97%, high purity , MAP kinase p38 alpha inhibitor, CAS No.623152-17-0, MAP kinase p38 alpha inhibitor

Item Number

B413913

• Synonyms: BMS-582949|623152-17-0|BMS 582949|BMS582949|UNII-CR743OME9E|CR743OME9E|PS540446|BMS582949 free base|PS-540446|4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide|CHEMBL1230065|623152-17-0 (free b
• Specifications & Purity: Moligand™, ≥97%
• Biochemical and Physiological Mechanisms: BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: MAP kinase p38 alpha inhibitor

Product Description

Information

BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.

Targets

p38 MAPK (Cell-free assay) 13 nM

In vitro

BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop.

In vivo

The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.