2. MAPK/ERK Pathway
  3. p38 MAPK
  4. BMS-582949

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.

For research use only. We do not sell to patients.

BMS-582949 Chemical Structure

BMS-582949 Chemical Structure

CAS No. : 623152-17-0

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Description

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[1].

IC50 & Target[1]

p38α

13 nM (IC50)

In Vivo

BMS-582949 (5 mg/kg, p.o., 90 min) reduces the LPS induced TNFα production significantly in murine models of acute inflammation from BALB/c female mice[1].
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 Compound 7k in Mice and Rats[1]

Compound 7k 在小鼠和大鼠中的药代动力学分析[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]

体外代谢分析[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.

Animal Model: murine models of acute inflammation from BALB/c female mice[1]
Dosage: 5 mg/kg
Administration: Oral gavage (p.o.), detection content at 90 min after LPS injection
Result: Reduced the TNFα production by 89% at 2 h, by 78% at 6 h before the LPS challenge.
Animal Model: Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
Dosage: 1, 10, 100 mg/kg, once daily (q.d)
Administration: Oral gavage (p.o.)
Result: Reduced paw swelling with dose-dependent, with efficacy observed at doses of 10 and 100 mg/kg.
Animal Model: Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
Dosage: 0-5 mg/kg, b.i.d
Administration: Oral gavage (p.o.)
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.
Clinical Trial
Molecular Weight

406.48

Formula

C22H26N6O2
CAS No.
SMILES

O=C(NCCC)C1=CN(N=CN=C2NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BMS-582949 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-582949623152-17-0BMS582949BMS 582949p38 MAPKorally activerat adjuvant arthritis (rat AA) modelsrheumatoid arthritisInhibitorinhibitorinhibit

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