A potent, selective EP4 receptor antagonist
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L-161,982

Item No. 10011565

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[[4'-[[3-butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
CAS Number
147776-06-5
Molecular Formula
C32H29F3N4O4S2
Formula Weight
654.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/ml
λmax
249 nm
SMILES
CCCCc1nn(c(=O)n1Cc1ccc(cc1)c1ccccc1S(=O)(=O)NC(=O)c1sccc1C)c1ccccc1C(F)(F)F
InChi Code
InChI=1S/C32H29F3N4O4S2/c1-3-4-13-28-36-39(26-11-7-6-10-25(26)32(33,34)35)31(41)38(28)20-22-14-16-23(17-15-22)24-9-5-8-12-27(24)45(42,43)37-30(40)29-21(2)18-19-44-29/h5-12,14-19H,3-4,13,20H2,1-2H3,(H,37,40)
InChi Key
MMDNKTXNUZFVKD-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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    25 mg

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    Product Description

    L-161,982 is a potent and selective EP4 receptor antagonist. It demonstrates selective binding to human EP4 receptors with a Ki value of 0.024 µM compared to other receptors of the prostanoid family, EP1, EP2, EP3, DP, FP, and IP, with Ki values of 17, 23, 1.9, 5.1, 5.6, and 6.7 µM, respectively.1 L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats1 and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.2 At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Machwate, M., Harada, S., Leu, C.T., et al. Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Mol. Pharmacol. 60(1), 36-41 (2001).

    2. Takayama, K., García-Gardeña, G., Sukhova, G.K., et al. Prostaglandin E2 suppresses chemokine production in human macrophages through the EP4 receptor. The Journal of Biological Chemisty 277(46), 44147-44154 (2002).

    3. Cherukuri, D.P., Chen, X.B.O., Goulet, A.C., et al. The EP4 receptor antagonist, L-161,982, blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells. Exp. Cell Res. 313(14), 2969-2979 (2007).

    Product Citations

    Lin, A., Wang, G., Zhao, H., et al. TLR4 signaling promotes a COX-2/PGE2/STAT3 positive feedback loop in hepatocellular carcinoma (HCC) cells. Oncoimmunology 5(2), e1074376 (2015).