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Submit ReviewL-798,106
Description: Potent and highly selective EP3 antagonist
Chemical Name: N-[(5-Bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide
Purity: ≥99% (HPLC)
Biological Activity for L-798,106
L-798,106 is a 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 for L-798,106
L-798,106 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for L-798,106
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L-798,106
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.64 | 100 |
Preparing Stock Solutions for L-798,106
The following data is based on the product molecular weight 536.44. 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 | 1.86 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 for L-798,106
References for L-798,106
References are publications that support the biological activity of the product.
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 lubipro. in rat and human stomach and colon. Br.J.Pharmacol. 154 126 PMID: 18332851
If you know of a relevant reference for L-798,106, please let us know.
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Keywords: L-798,106, L-798,106 supplier, Potent, selective, EP3, antagonists, Receptors, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L798106, 3342, Tocris Bioscience
7 Citations for L-798,106
Citations are publications that use Tocris products. Selected citations for L-798,106 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
Zhu (2018) Prostaglandin receptor EP3 regulates cell proliferation and migration with impact on survival of endometrial cancer patients. Oncotarget 9 982 PMID: 29416671
Ye et al (2018) Prostaglandin E2 receptor 3 signaling is induced in placentas with unexplained recurrent pregnancy losses. Endocr Connect 7 749 PMID: 29700097
Fernández-Galilea et al (2012) Effects of lipoic acid on lipolysis in 3T3-L1 adipocytes. J Lipid Res 53 2296 PMID: 22941773
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Tunaru et al (2012) Castor oil induces laxation and uterus contraction via ricinoleic acid activating prostaglandin EP3 receptors. Cell Commun Signal 109 9179 PMID: 22615395
Yang et al (2015) Exposure to 50 Hz magnetic field modulates GABAA currents in cerebellar granule neurons through an EP receptor-mediated PKC pathway. J Cell Mol Med 19 2413 PMID: 26176998
Do you know of a great paper that uses L-798,106 from Tocris? Please let us know.
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