- BMS582949
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- $79.00
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2026-04-20
- CAS:623152-17-0
- Purity: 98.43%
- Supply Ability: 10g
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| | BMS 582949 Basic information |
| Product Name: | BMS 582949 | | Synonyms: | BMS 582949;BMS582949(HCl);4-[[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;4-[5-(cyclopropylcarbamoyl)-2-methylanilino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;CS-2900;BMS 582949; BMS582949;PS540446;Pyrrolo[2,1-f][1,2,4]triazine-6-carboxamide, 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propyl- | | CAS: | 623152-17-0 | | MF: | C22H26N6O2 | | MW: | 406.48 | | EINECS: | 604-604-1 | | Product Categories: | | | Mol File: | 623152-17-0.mol |  |
| | BMS 582949 Chemical Properties |
| 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 |
| | BMS 582949 Usage And Synthesis |
| 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 | | 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. |
| | BMS 582949 Preparation Products And Raw materials |
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