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Description: Selective EP4 receptor antagonist
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% (HPLC)
Citations (3)

Biological Activity for L-161,982

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.

Compound Libraries for L-161,982

L-161,982 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for L-161,982

M. Wt 654.72
Formula C32H29F3N4O4S2
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 147776-06-5
PubChem ID 9961192
Smiles CCCCC1=NN(C(=O)N1CC1=CC=C(C=C1)C1=C(C=CC=C1)S(=O)(=O)NC(=O)C1=C(C)C=CS1)C1=C(C=CC=C1)C(F)(F)F

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.

Solubility Data for L-161,982

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 65.47 100

Preparing Stock Solutions for L-161,982

The following data is based on the product molecular weight 654.72. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.53 mL 7.64 mL 15.27 mL
5 mM 0.31 mL 1.53 mL 3.05 mL
10 mM 0.15 mL 0.76 mL 1.53 mL
50 mM 0.03 mL 0.15 mL 0.31 mL

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Product Datasheets for L-161,982

Certificate of Analysis / Product Datasheet
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References for L-161,982

References are publications that support the biological activity of the product.

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

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

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

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

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Keywords: L-161,982, L-161,982 supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Receptors, 2514, Tocris Bioscience

3 Citations for L-161,982

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

Sun et al (2011) Lubiprostone reverses the inhibitory action of mor. on mucosal secretion in human small intestine. Dig Dis Sci 56 330 PMID: 21181441

Guillem-Llobat et al (2016) Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells. Oncotarget 7 32462 PMID: 27074574

Do you know of a great paper that uses L-161,982 from Tocris? Please let us know.

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