Biological Activity
Potent and highly selective prostanoid EP3 receptor antagonist (Ki values are 0.3, 916, > 5000 and > 5000 nM at EP3, EP4, EP1 and EP2 respectively). Attenuates sulprostone-induced inhibition of EFS-evoked twitch and contractile responses in vivo.
Compound Libraries
L-798,106 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 536.44 |
| Formula | C27H22BrNO4S |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 244101-02-8 |
| PubChem ID | 15551229 |
| InChI Key | ODTKFNUPVBULRJ-NTCAYCPXSA-N |
| Smiles | O=C(NS(C4=C(OC)C=CC(Br)=C4)(=O)=O)/C=C/C1=CC=CC=C1CC3=CC2=CC=CC=C2C=C3 |
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 | 53.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 536.44. 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 | 1.86 mL | 9.32 mL | 18.64 mL |
| 5 mM | 0.37 mL | 1.86 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Juteau et al (2001) Structure-activity relationships of cinnamic acylsulfonamide analogues on human EP3 prostanoid receptor. Bioorg.Med.Chem. 9 1977 PMID: 11504634
Clarke et al (2004) E-ring 8-isoprostanes inhibit ACh release from parasympathetic nerves innervating guinea-pig trachea through agonism of prostanoid receptors of the EP3-subtype. Br.J.Pharmacol. 141 600 PMID: 14744812
Bassil et al (2008) Activation of prostaglandin EP receptors by lubiprostone in rat and human stomach and colon. Br.J.Pharmacol. 154 126 PMID: 18332851
Keywords: L-798,106, supplier, Potent, selective, EP3, antagonists, Receptors, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L798106, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
