L-161,982

Cat. No. 2514

L-161,982 C32H29F3N4O4S2 [147776-06-5]

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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

Biological Activity

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 in formalin-injected mice.

Technical Data

M.Wt:
654.72
Formula:
C32H29F3N4O4S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
147776-06-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Balzary et al (2006) Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2. J.Pharmacol.Exp.Ther. 317 806. PMID: 16464966.

Oliva et al (2006) Role of periaqueductal grey prostaglandin receptors in formalin-induced hyperalgesia. Eur.J.Pharmacol. 530 40. PMID: 16360148.

Machwate et al (2001) Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Mol.Pharmacol. 60 36. PMID: 11408598.

If you know of a relevant reference for L-161,982 please let us know.

Citations are publications that use Tocris products. Selected citations for L-161,982 include:

Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10. PMID: 21955547.

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Keywords: L-161,982, supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Tocris Bioscience, Prostanoid Receptor Antagonist products

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