BMS-582949 HCl

SKU: orb1223000

Description

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.

Key Properties

• CAS Number: 912806-16-7
• MW: 442.95
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₇ClN₆O₂
• SMILES: n12ncnc(c1c(c(c2)C(=O)NCCC)C)Nc1c(ccc(c1)C(=O)NC1CC1)C.Cl
• Target: PDK
• Solubility: DMSO : ≥ 35 mg/mL; 79.02 mM

Bioactivity

• 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. 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PDK