A potent inhibitor of p38α MAP kinase
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LY2228820 (mesylate)

Item No. 23259

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[2-(1,1-dimethylethyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)-3H-imidazo[4,5-b]pyridin-2-amine, dimethanesulfonate
CAS Number
862507-23-1
Synonyms
  • LSN2322600
Molecular Formula
C24H29FN6 • 2CH3SO3H
Formula Weight
612.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
321 nm
SMILES
NC1=NC2=CC=C(C3=C(C4=CC=C(F)C=C4)N=C(C(C)(C)C)N3)N=C2N1CC(C)(C)C.OS(=O)(C)=O.OS(=O)(C)=O
InChi Code
InChI=1S/C24H29FN6.2CH4O3S/c1-23(2,3)13-31-20-17(28-22(31)26)12-11-16(27-20)19-18(14-7-9-15(25)10-8-14)29-21(30-19)24(4,5)6;2*1-5(2,3)4/h7-12H,13H2,1-6H3,(H2,26,28)(H,29,30);2*1H3,(H,2,3,4)
InChi Key
NARMJPIBAXVUIE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $160

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    10 mg

    $303

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    25 mg

    $629

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    Product Description

    LY2228820 is a potent inhibitor of p38α MAP kinase (IC50 = 7 nM for human recombinant p38α).1 It inhibits LPS-induced TNF-α production in murine peritoneal macrophages and reduces phosphorylation of MAPKAPK-2 (MK2) in RAW 264.7 cells (IC50s = 5.2 and 34.3 nM, respectively). LY2228820 inhibits TNF-α production in LPS-treated mice and reduces paw swelling and cartilage destruction in a rat model of chronic inflammation with threshold minimum 50% doses (TMED50) values of <1, 1.5, and 1.5 mg/kg, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mader, M., de Dios, A., Shih, C., et al. Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties. Bioorg. Med. Chem. Lett. 18(1), 179-183 (2008).