L-798,106

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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)
Datasheet
Citations (7)
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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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:

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

Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349

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

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


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