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L-161,982 (CAS 147776-06-5) LS-H60

EP4 receptor antagonist
LS-H60-1 / 1 mg / $175
LS-H60-5 / 5 mg / $245
LS-H60-10 / 10 mg / $315
LS-H60-50 / 50 mg / $995
USA Shipment Only
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Description: Prostaglandin E2 (PGE2) exerts its effects through four separate G coupled-protein receptors (EP1-4). 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. L-161,982 at 10 mg/kg/day suppresses PGE2-stimulated bone formation in young rats and at 100 nM reverses the anti-inflammatory action of PGE2 in LPS-activated human macrophages. At 10 µM L-161982 blocks PGE2-induced cell proliferation in HCA-7 colon cancer cells. H60_ChemicalStructureImage.png
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
 
biochemical, chemical, antagonist
LS-H60
147776-06-5
C32H29F3N4O4S2
≥95%
A crystalline solid
 
CCCCc1nn(c(=O)n1Cc1ccc(cc1)c1ccccc1S(=O)(=O)NC(=O)c1sccc1C)c1ccccc1C(F)(F)F
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)
MMDNKTXNUZFVKD-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: PTGER4 / EP4 related products

Usage Information

L-161,982 is supplied as a crystalline solid. A stock solution may be made by dissolving the L-161,982 in an organic solvent purged with an inert gas. L-161,982 is soluble in organic solvents such as DMSO and dimethyl formamide. The solubility of L-161,982 in these solvents is approximately 10 mg/ml. If aqueous stock solutions are required for biological experiments, they can best be prepared by diluting the organic solvent into aqueous buffers or isotonic saline. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

References:
  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.-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, 2969-2979 (2007).

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