BMS-582949 hydrochloride - 10mM in DMSO , CAS No.912806-16-7

CAS: 912806-16-7 Cat. No.: B656025 Peso molecular: 442.94 PubChem CID: 11848302

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC 50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease

In Vitro

BMS-582949 displays a p38α IC 50 of 13 nM and a cellular TNFα IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

IC50& Target:p38α MAPK 13 nM (IC 50 ) TNFα 50 nM (IC 50 , in cells)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC 50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.

Condiciones de almacenamiento de almacenamiento

Desiccated, Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CCCNC(=O)C1=CN2C(=C1C)C(=NC=N2)NC3=C(C=CC(=C3)C(=O)NC4CC4)C.Cl
• CAS alternativo: 912806-16-7
• PubChem CID: 11848302
• Peso molecular: 442.94