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BMS-582949

Cat. No. M9160

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BMS-582949 Structure
Synonym:

PS540446; BMS582949 free base

Size Price Availability Quantity
2mg USD 207  USD207 In stock
5mg USD 297  USD297 In stock
10mg USD 537  USD537 In stock
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Quality Control & Documentation
Biological Activity

BMS-582949 inhibits both p38 kinase activity and activation 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 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. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.

Chemical Information
Molecular Weight 406.48
Formula C22H26N6O2
CAS Number 623152-17-0
Solubility (25°C) DMSO: ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Emami H, et al. Atherosclerosis. The effect of BMS-582949, a P38 mitogen-activated protein kinase (P38 MAPK) inhibitor on arterial inflammation: a multicenter FDG-PET trial.

[2] Liu C, et al. J Med Chem. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

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Keywords: BMS-582949, PS540446; BMS582949 free base supplier, p38 MAPK, inhibitors, activators

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