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Submit ReviewL-161,982
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)
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 |
| InChI Key | MMDNKTXNUZFVKD-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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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