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L-161,982

Cayman Chemical Item Number 10011565

(CAS 147776-06-5)

L-161,982 (CAS 147776-06-5)

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Description

Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4).1 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.2 L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats2 and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages.3 At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells.4

1 Coleman, R.A., Smith, W.L., and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 46 205-229 (1994).

2 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).

3 Takayama, K., García-Gardeña, G., Sukhova, G.K., et al. Prostaglandin E2 suppresses chemokine production in human macrophages through the EP4 receptor. J Biol Chem 277(46) 44147-44154 (2002).

4 Cherukuri, D.P., Chen, X.B.O., Goulet, A., 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 2969-2979 (2007).

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 654.2
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCCCc1nn(c(=O)​n1Cc1ccc(cc1)​c1ccccc1S(=O)​(=O)​NC(=O)​c1sccc1C)​c1ccccc1C(F)​(F)​F

Background Reading

Cherukuri, D.P., Chen, X.B.O., Goulet, A., 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 2969-2979 (2007).

Takayama, K., García-Gardeña, G., Sukhova, G.K., et al. Prostaglandin E2 suppresses chemokine production in human macrophages through the EP4 receptor. J Biol Chem 277(46) 44147-44154 (2002).

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).

Coleman, R.A., Smith, W.L., and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 46 205-229 (1994).

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Size Price Quantity Subtotal
1 mg $27.00 $0.00
5 mg $122.00 $0.00
10 mg $216.00 $0.00
50 mg $945.00 $0.00
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Cart Total $0.00

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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