A selective p38 MAPK inhibitor
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PH-797804

Item No. 20244

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethyl-benzamide
CAS Number
586379-66-0
Molecular Formula
C22H19BrF2N2O3
Formula Weight
477.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12.5 mg/mLDMSO: 14 mg/mLDMSO:PBS (pH 7.2)(1:5): 0.16 mg/mLEthanol: 2.5 mg/mL
λmax
219, 309 nm
SMILES
FC1=CC(F)=C(COC2=C(Br)C(N(C3=C(C)C=CC(C(NC)=O)=C3)C(C)=C2)=O)C=C1
InChi Code
InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28)
InChi Key
KCAJXIDMCNPGHZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    PH-797804 is an inhibitor of p38α MAPK with an IC50 value of 26 nM in a cell-free assay.1,2 It is 4-fold more selective for p38α compared to p38β and does not inhibit JNK2 or ERK at concentrations up to 1 µM.1 PH-797804 treatment for 10 days in vivo demonstrates anti-inflammatory activity in chronic inflammatory disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and collagen-induced arthritis in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hope, H.R., Anderson, G.D., Burnette, B.L., et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J. Pharmacol. Exp. Ther. 331(3), 882-895 (2009).

    2. Goldstein, D.M., Kuglstatter, A., Lou, Y., et al. Selective p38α inhibitors clinically evaluated for the treatment of chronic inflammatory disorders. J. Med. Chem. 53, 2345-2353 (2010).