| Identification | Back Directory | [Name]
BMS 582949 | [CAS]
623152-17-0 | [Synonyms]
CS-2900
PS540446
BMS 582949
BMS582949(HCl)
BMS 582949; BMS582949
4-[5-(cyclopropylcarbamoyl)-2-methylanilino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide
4-[[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide
Pyrrolo[2,1-f][1,2,4]triazine-6-carboxamide, 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propyl- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C22H26N6O2 | [MDL Number]
MFCD18633248 | [MOL File]
623152-17-0.mol | [Molecular Weight]
406.48 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
A crystalline solid | [InChIKey]
GDTQLZHHDRRBEB-UHFFFAOYSA-N | [SMILES]
N12C=C(C(NCCC)=O)C(C)=C1C(NC1=CC(C(NC3CC3)=O)=CC=C1C)=NC=N2 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
bms-582949 is a p38 mapk inhibitorp38r map kinase plays a key role in regulating the biosynthesis of various inflammatory cytokines, such as tumor necrosis factor alpha and interleukin-1β. thus, p38r inhibitors are considered as a promising therapy for inflammatory disease treatment. | [in vitro]
bms-582949 was found to be 450-fold selective over jnk2, a map kinase involved in inflammation, and 190-fold selective against raf. moreover, the binding mode of bms-582949 with p38r was further demonstrated by x-ray crystallographic analyses [1]. | [in vivo]
in a pseudoestablished rat adjuvant arthritis model, bms-582949 at doses of 10 and 100 mg/kg was found to display dose-dependent reduction in paw swelling with qd dosing. in addition, with bid dosing at doses of 1 and 5 mg/kg, bms-582949 showed improved efficacy, resulting in great reduction in paw swelling. moreover, the statistically significant reduction in paw swelling was also observed with the treatment of bms-582949 at doses as low as 0.3 mg/kg bid [1]. | [target]
| Target | Value | p38 MAPK
(Cell-free assay) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 13 nM
| [IC 50]
13 nm | [storage]
Store at -20°C | [References]
[1]. liu c, et al. discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl- n-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (bms-582949), a clinical p38α map kinase inhibitor for the treatment of inflammatory diseases. j med chem. 2010 sep 23;53(18):6629-39.
[2]. emami h, et al. the effect of bms-582949, a p38 mitogen-activated protein kinase (p38 mapk) inhibitor on arterial inflammation: a multicenter fdg-pet trial. atherosclerosis. 2015 jun;240(2):490-6. |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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