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BMS-582949 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-582949 HCl图片
CAS NO:912806-16-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)442.94
FormulaC22H27ClN6O2
CAS No.623152-17-0 (HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 35 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILESO=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC.[H]Cl
SynonymsPS540446 HCl; BMS-582949; BMS 582949; BMS582949; PS-540446; PS 540446; PS540446
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: 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.


Cell Assay: BMS-582949 inhibits both p38 kinase activity and activation of p38. 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.

In VivoThe 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 μMoh. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.
Animal modelMouse
Formulation & DosageOral dose of 10 mg/kg
ReferencesJ Med Chem. 2010 Sep 23;53(18):6629-39; Arthritis Rheum. 2010, 62 Suppl 10:1513.