A potent mPGES-1 inhibitor
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PF-9184

Item No. 18904

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
CAS Number
1221971-47-6
Molecular Formula
C21H14Cl2N2O4S
Formula Weight
461.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 15 mg/ml
λmax
269, 335 nm
SMILES
OC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O
InChi Code
InChI=1S/C21H14Cl2N2O4S/c22-16-10-7-13(11-17(16)23)12-5-8-14(9-6-12)24-21(27)19-20(26)15-3-1-2-4-18(15)30(28,29)25-19/h1-11,25-26H,(H,24,27)
InChi Key
VGACSWBJQLLJFB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $120

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    10 mg

    $167

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    25 mg

    $354

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    Product Description

    Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).1 Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.2 PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).3 It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jakobsson, P.J., Thorén, S., Morgenstern, R., et al. Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target. Proc. Natl. Acad. Sci. USA 96(13), 7220-7225 (1999).

    2. Stichtenoth, D.O., Thorén, S., Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. J. Immunol. 167(1), 469-474 (2001).

    3. Mbalaviele, G., Pauley, A.M., Shaffer, A.F., et al. Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochem. Pharmacol. 79(10), 1445-1454 (2010).

    4. Chang, H.H., and Meuillet, E.J. Identification and development of mPGES-1 inhibitors: Where we are at? Future Med. Chem. 3(15), 1909-1934 (2011).

    5. Korotkova, M., and Jakobsson, P.J. Microsomal prostaglandin E synthase-1 in rheumatic diseases. Front. Pharmacol. 1, 146 (2011).