L-798106
Based on 1 publication(s) in Google Scholar
L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.91%
- No. CAS: 244101-02-8
- Fòrmula: C27H22BrNO4S
- Peso molecular:536.44
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) L-798106
More
Actividad biológica
Descripciòn
IC50 & Target
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EP3 0.3 nM (Ki) |
EP4 916 nM (Ki) |
EP1 >5000 nM (Ki) |
EP2 >5000 nM (Ki) |
In Vitro
L-798106 (200 nM) inhibits electrical field stimulation-induced contractile responses[2].
L-798106 (10 μM) inhibits electrical field stimulation-evoked ACh release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Guinea-pig vas deferens
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Concentration:200 nM
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Incubation Time:
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Result:Showed an apparent pA2 of 7.48±0.25.
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Cell Line:Guinea-pig tracheal smooth muscle
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Concentration:10 μM
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Incubation Time:
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Result:Attenuated significantly the inhibitory effect of all agents tested (in % inhibition of EFS-induced release: 8-iso-PGE1 from 56.9 to 8.6; 8-iso-PGE2 from 51.6 to 9.2; PGE2 from 61.2 to 2.9; sulprostone from 55.9 to 18.8).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male db/db mice[3]
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Dosage:50 and 100 μg/kg
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Administration:Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks
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Result:Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice.
Chemical Information
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No. CAS 244101-02-8
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Appearance Solid
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Peso molecular 536.44
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Fòrmula C27H22BrNO4S
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Color White to off-white
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SMILES
O=C(NS(=O)(C1=CC(Br)=CC=C1OC)=O)/C=C/C2=CC=CC=C2CC3=CC=C4C=CC=CC4=C3
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Synonyms
CM9; GW671021
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Neurogastroenterol Motil
Shugan Decoction Ameliorated WAS-Induced Abnormal Colonic Motility in Rats by Inhibiting Colonic TRPV4-PGE2 Signaling. [Abstract]2025 Dec;37(12):e70104. PMID: 40545667
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (46.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Juteau H, et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg Med Chem. 2001 Aug;9(8):1977-84. [Content Brief]
[2]. Deborah L Clarke, et al. 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. 2004 Feb;141(4):600-9. [Content Brief]
[3]. Pei-Chi Chan, et al. Importance of adipocyte cyclooxygenase-2 and prostaglandin E2-prostaglandin E receptor 3 signaling in the development of obesity-induced adipose tissue inflammation and insulin resistance. FASEB J. 2016 Jun;30(6):2282-97. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8641 mL | 9.3207 mL | 18.6414 mL | 46.6035 mL |
| 5 mM | 0.3728 mL | 1.8641 mL | 3.7283 mL | 9.3207 mL | |
| 10 mM | 0.1864 mL | 0.9321 mL | 1.8641 mL | 4.6604 mL | |
| 15 mM | 0.1243 mL | 0.6214 mL | 1.2428 mL | 3.1069 mL | |
| 20 mM | 0.0932 mL | 0.4660 mL | 0.9321 mL | 2.3302 mL | |
| 25 mM | 0.0746 mL | 0.3728 mL | 0.7457 mL | 1.8641 mL | |
| 30 mM | 0.0621 mL | 0.3107 mL | 0.6214 mL | 1.5535 mL | |
| 40 mM | 0.0466 mL | 0.2330 mL | 0.4660 mL | 1.1651 mL |
L-798106 Related Classifications
HY-15274 Related Classifications
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