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.
Compound Libraries
L-161,982 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 65.47 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 654.72. Batch specific molecular weights may vary from batch to batch due to solvent 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
References
References are publications that support the products' biological activity.
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
Keywords: L-161,982, supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
