A p38α MAP kinase inhibitor
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BMS 582949

Item No. 22892

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propyl-pyrrolo[2,1-f][1,2,4]triazine-6-carboxamide
CAS Number
623152-17-0
Molecular Formula
C22H26N6O2
Formula Weight
406.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): Slightly soluble
λmax
253 nm
SMILES
CC1=CC=C(C(NC2CC2)=O)C=C1NC3=NC=NN4C3=C(C)C(C(NCCC)=O)=C4
InChi Code
InChI=1S/C22H26N6O2/c1-4-9-23-22(30)17-11-28-19(14(17)3)20(24-12-25-28)27-18-10-15(6-5-13(18)2)21(29)26-16-7-8-16/h5-6,10-12,16H,4,7-9H2,1-3H3,(H,23,30)(H,26,29)(H,24,25,27)
InChi Key
GDTQLZHHDRRBEB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

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    10 mg

    $270

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    25 mg

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    Product Description

    BMS 582949 is an orally bioavailable p38α MAP kinase inhibitor (IC50 = 13 nM in an enzyme assay).1 It also inhibits TNF-α production in human peripheral blood mononuclear cells (PBMC; IC50 = 50 nM). When administered at a dose of 5 mg/kg in mice, it decreases LPS-induced TNF-α production up to 89% compared to vehicle. BMS 582949 reduces paw swelling in a rat adjuvant arthritis model when administered once per day (1, 10, or 100 mg/kg) or twice per day (1 or 5 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, C., Lin, J., Wrobleski, S.T., 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. 53(18), 6629-6639 (2010).

    Product Citations

    Maronde, E. Trehalose activates CRE-dependent transcriptional signaling in HT22 mouse hippocampal neuronal cells: A central role for PKA without cAMP elevation. Front. Mol. Neurosci. 11:386, (2018).