L-161,982
Chemical 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
Purity: ≥99%
Biological Activity
L-161,982 is an EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively). Suppresses PGE2-induced bone formation in rats and prevents the nociceptive response induced by Misoprostol (Cat. No. 2297) in formalin-injected mice.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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PGE2 maintains self-renewal of human adult stem cells via EP2-mediated autocrine signaling and its production is regulated by cell-to-cell contact
Byung-Chul Lee
Sci Rep, 2016;6(0):26298. -
Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2.
Machwate et al.
Mol.Pharmacol., 2001;60:36 -
Role of periaqueductal grey prostaglandin receptors in formalin-induced hyperalgesia.
Oliva et al.
Eur.J.Pharmacol., 2006;530:40 -
Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2.
Balzary et al.
J.Pharmacol.Exp.Ther., 2006;317:806
Product Datasheets
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Citations for L-161,982
The citations listed below are publications that use Tocris products. Selected citations for L-161,982 include:
3 Citations: Showing 1 - 3
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Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells.
Authors: Guillem-Llobat Et al.
Oncotarget 2016;7:32462
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Lubiprostone reverses the inhibitory action of mor. on mucosal secretion in human small intestine.
Authors: Sun Et al.
Dig Dis Sci 2011;56:330
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Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice.
Authors: Chia Et al.
BMC Pharmacol 2011;11:10
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