BMS-582949
Based on 2 publication(s) in Google Scholar
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis.
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- No. CAS: 623152-17-0
- Fòrmula: C22H26N6O2
- Peso molecular:406.48
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Actividad biológica
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p38α 13 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
50 nM
Compound: 7k
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS challenge measured after 6 hrs by ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS challenge measured after 6 hrs by ELISA
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[PMID: 20804198] |
BMS-582949 (0.3-100 mg/kg, p.o., q.d/b.i.d) reduces paw swelling significantly[1].
BMS-582949 intravenous injection (i.v.) dissolution protocol uses 25% NMP, 33% PEG 400, 9% PG, and 33% water as a vehicle[1].
BMS-582949 oral gavage (p.o.) dissolution protocol uses PEG 400 as a vehicle[1].
Pharmacokinetic Properties of BMS-582949 (Compound 7k) in Mice and Rats[1]
| mouse | rat | |
| %Fpo | 90 | 60 |
| Cmax(μM) | 15.3 | 7.0 |
| Tmax(h) | 1.0 | 1.5 |
| T1/2(h) | 2.6 | 4.0 |
| MRT (h) | 3.3 | 3.4 |
| CL (mL/min/kg) | 4.4 | 5.4 |
| Vss(L/kg) | 0.9 | 1.1 |
| AUC0-8 h(μM h) | 75.5 | |
| AUC0-24 h(μM h) | 45.4 |
In Vitro Profile of 7k[1]
| profiling assays | results |
| liver microsome metabolic rate (nmol/min/mg) | mouse: 0.011 rat: 0.008 human: 0.013 |
| hepatocyte metabolic rate (nmol/min/million cells) | mouse: 0.006 rat: 0.015 human: 0.015 |
| P450 IC50(μM) | >40 for 1A2, 2C9 2C19, and 2D6 18-40 for 3A4 |
| Caco-2 permeability (nm/s) | 121-134 |
| serum protein binding (%) | mouse: 86.3 rat: 89.7 human: 81.5 |
| Ames | negative in T98 and T100±S9 activation |
| SOS chromotest | negative |
| HHA IC50(μM) | >138 |
| hERG inhibition | 16% at 30 μM |
| kinase selectivity | >2000 fold over 57 diverse kinase 450 fold over Jnk2 190 fold over Raf 5 fold over p38α |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:murine models of acute inflammation from BALB/c female mice[1]
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Dosage:5 mg/kg
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Administration:Oral gavage (p.o.), detection content at 90 min after LPS injection
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Result:Reduced the TNFα production by 89% at 2 h, by 78% at 6 h before the LPS challenge.
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Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
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Dosage:1, 10, 100 mg/kg, once daily (q.d)
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Administration:Oral gavage (p.o.)
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Result:Reduced paw swelling with dose-dependent, with efficacy observed at doses of 10 and 100 mg/kg.
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Animal Model:Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
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Dosage:0-5 mg/kg, b.i.d
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Administration:Oral gavage (p.o.)
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Result:Improved efficacy markedly of reduction in paw swelling at doses of 1 and 5 mg/kg.
Reduced paw swelling significantly at doses as low as 0.3 mg/kg.
Chemical Information
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No. CAS 623152-17-0
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Peso molecular 406.48
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Fòrmula C22H26N6O2
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SMILES
O=C(NCCC)C1=CN(N=CN=C2NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Oncol Res
Therapeutic Targeting PLK1 by ON-01910.Na Is Effective in Local Treatment of Retinoblastoma. [Abstract]2021 Sep 7;28(7):745-761. PMID: 33573708
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