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| Targets |
L-798,106 targets the prostaglandin E2 (PGE2) receptor subtype EP3, which is a G protein-coupled receptor. It acts as a highly selective antagonist, binding to the EP3 receptor and blocking the effects of PGE2. The compound exhibits remarkable selectivity, with Ki values of 0.3 nM at EP3, 916 nM at EP4, and >5,000 nM at EP1 and EP2. This indicates that L-798,106 is more than 3,000-fold selective for EP3 over EP1 and EP2, and over 3,000-fold selective for EP3 over EP4.
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| ln Vitro |
The contractile response brought on by an electric field stimulation is inhibited by L-798106 (200 nM) [2]. Acetylcholine release triggered by electric field stimulation is inhibited by L-798106 (10 μM) [2].
In vitro, L-798,106 is a potent and highly selective EP3 receptor antagonist. Its activity is demonstrated by its ability to block the EP3 agonist activity of sulprostone at a concentration of 0.2 µM. The compound's high affinity for the EP3 receptor, with a Ki of 0.3 nM, confirms its potent antagonism. These in vitro activities confirm its role as a specific EP3 receptor antagonist. |
| ln Vivo |
In db/db mice, L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 weeks) reduces AT inflammation and systemic insulin resistance [3].
Detailed in vivo activity data for L-798,106 are not extensively reported in the available literature. However, as a potent and selective EP3 receptor antagonist, it is expected to have in vivo efficacy in models of pain, inflammation, and other PGE2-mediated conditions. The compound's high selectivity suggests it could be used to specifically study the role of the EP3 receptor in these processes without affecting other EP receptor subtypes. |
| Enzyme Assay |
Non-cell-based receptor binding assays for L-798,106 involve radioligand binding studies using membrane preparations from cells expressing the human EP3, EP4, EP1, and EP2 receptors. The receptor is incubated with a radiolabeled PGE2 ligand and varying concentrations of L-798,106. Its binding affinity (Ki) is determined by measuring the displacement of the radiolabeled ligand. Selectivity profiling against other EP receptor subtypes is performed to confirm specificity.
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| Cell Assay |
Cell viability assay [2]
Cell Types: Guinea pig vas deferens Tested Concentrations: 200 nM Incubation Duration: Experimental Results: Apparent pA2 is 7.48±0.25. Cell viability assay [2] Cell Types: Guinea pig tracheal smooth muscle Tested Concentrations: 10 μM Incubation Duration: Experimental Results: The inhibitory effects of all tested drugs were Dramatically attenuated (% inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 2-iso- PGE2 increased from 51.6 to 8.6; 8-iso-PGE2 increased from 51.6 to 9.2; PGE2 increased from 61.2 to 2.9; sulprostone increased from 55.9 to 18.8. Cellular assays for L-798,106 are performed using cells expressing EP3 receptors. Cells are treated with the compound at various concentrations, followed by stimulation with a PGE2 or an EP3 receptor agonist. Downstream signaling, such as cAMP inhibition or calcium mobilization, is measured. The compound's ability to inhibit agonist-induced signaling is quantified. IC50 values for receptor antagonism are determined from dose-response curves. |
| Animal Protocol |
Animal/Disease Models: Male db/db mice [3]
Doses: 50 and 100 μg/kg Route of Administration: po (oral gavage); 50 and 100 μg/kg; one time/day; 8 weeks Experimental Results: Inhibited fasting of db/db mice An increase in blood sugar levels. Suppression of increased pro-inflammatory gene expression in adipocytes isolated from epididymal AT of db/db mice. In vivo animal models for L-798,106 would be required to assess its therapeutic potential. Based on its mechanism as an EP3 receptor antagonist, relevant models could include pain models (e.g., inflammatory pain, neuropathic pain) and models of central nervous system function. The compound would be administered via appropriate routes, and behavioral and physiological parameters would be measured. Detailed protocols are not extensively reported in the available literature. |
| ADME/Pharmacokinetics |
L-798,106 has a molecular weight of 536.44 g/mol and a molecular formula of C₂₇H₂₂BrNO₄S. Its CAS number is 244101-02-8. The compound is supplied as a crystalline solid with a purity of ≥95%. It is soluble in DMSO (10 mg/mL) and DMF (20 mg/mL). Storage conditions: -20°C. The compound is stable for at least 4 years when stored as a powder under recommended conditions.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L-798,106 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
L-798106 is an N-sulfonylformamide formed by the condensation of the carboxyl group of o-naphth-2-ylcinnamic acid and the sulfonamide group of 5-bromo-2-methoxybenzenesulfonamide. It is a selective antagonist of the prostaglandin receptor EP3 (the receptor for prostaglandin E2 (PGE2)). It functions as a prostaglandin receptor antagonist. It is an N-sulfonylformamide belonging to the bromobenzene class and aromatic ether class of compounds.
L-798,106 is also known as CM 9 and GW 671021. It is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively. It blocks the EP3 agonist activity of sulprostone at 0.2 µM. It is used in prostanoid receptor signaling studies. Its CAS number is 244101-02-8. |
| Molecular Formula |
C27H22BRNO4S
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| Molecular Weight |
536.44
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| Exact Mass |
535.045
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| CAS # |
244101-02-8
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| PubChem CID |
15551229
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| Appearance |
White to off-white solid powder
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| Density |
1.425±0.06 g/cm3(Predicted)
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| LogP |
7.191
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
810
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C(C=C1)Br)S(=O)(=O)NC(=O)/C=C/C2=CC=CC=C2CC3=CC4=CC=CC=C4C=C3
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| InChi Key |
ODTKFNUPVBULRJ-NTCAYCPXSA-N
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| InChi Code |
InChI=1S/C27H22BrNO4S/c1-33-25-14-13-24(28)18-26(25)34(31,32)29-27(30)15-12-21-7-3-5-9-23(21)17-19-10-11-20-6-2-4-8-22(20)16-19/h2-16,18H,17H2,1H3,(H,29,30)/b15-12+
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| Chemical Name |
(E)-N-(5-bromo-2-methoxyphenyl)sulfonyl-3-[2-(naphthalen-2-ylmethyl)phenyl]prop-2-enamide
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| Synonyms |
L798,106; L 798,106; L-798,106
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~18.64 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8641 mL | 9.3207 mL | 18.6414 mL | |
| 5 mM | 0.3728 mL | 1.8641 mL | 3.7283 mL | |
| 10 mM | 0.1864 mL | 0.9321 mL | 1.8641 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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