"目錄號(hào): HY-14305A
BMS-582949鹽酸鹽是一種新型的選擇性p38α MAPK抑制劑, IC50值為13 nM。
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生物活性
Description
BMS-582949 hydrochloride is a novel highly selective p38α MAPK inhibitor, inhibits p38α with IC50 of 13 nM. IC50 value: 13 nM[1]Target: p38αin vitro: BMS-582949 does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 with IC50values >40 μM. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. BMS-582949 is also 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective over Raf[1].BMS-582949 is a novel highly selective p38α MAPK inhibitor [2]. 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[1].
Clinical Trial
Bristol-Myers Squibb
Rheumatoid Arthritis
November 2005
Phase 1
Bristol-Myers Squibb
Psoriasis
August 2007
Phase 2
Bristol-Myers Squibb
Rheumatoid Arthritis, NOS
March 2008
Phase 2
Bristol-Myers Squibb
Vascular Diseases
December 2008
Phase 2
Bristol-Myers Squibb
Rheumatoid Arthritis
November 2005
Phase 1
Bristol-Myers Squibb
Psoriasis
August 2007
Phase 2
Bristol-Myers Squibb
Rheumatoid Arthritis, NOS
March 2008
Phase 2
Bristol-Myers Squibb
Vascular Diseases
December 2008
Phase 2
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