BMS-582949 HCl

Research use only, not for human use.

The BMS-582949 hydrochloride is a highly specific p38α MAPK inhibitor (IC50: 13 nM).

The BMS-582949 hydrochloride is a highly specific p38α MAPK inhibitor (IC50: 13 nM).(In Vitro):BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.BMS-582949 is a weak inhibitor of CYP3A4 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.(In Vivo):BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency.

BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.BMS-582949 is a weak inhibitor of CYP3A4 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 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency. Animal Model:Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model.Dosage:1, 10, 100 mg/kg.Administration:Orally once daily (from day 11 to day 19).Result:Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.

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PI3K/Akt/mTOR signaling

PDK

p38α

Inflammation/Immunology

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912806-16-7

442.95

C22H27ClN6O2

>98% (HPLC)

DMSO : ≥ 35 mg/mL; 79.02 mM

n12ncnc(c1c(c(c2)C(=O)NCCC)C)Nc1c(ccc(c1)C(=O)NC1CC1)C.Cl

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(-20℃)

With Ice Pack

≥ 2 years