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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.91%
- CAS 番号: 244101-02-8
- 分子式: C27H22BrNO4S
- 分子量:536.44
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Prostaglandin E2 (Standard) -
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Prostaglandin E2 (GMP)Inflammatory Mediator (GMP)
MedChemExpress（MCE）の使用を引用している文献 L-798106
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生物活性
製品説明
IC50 & Target
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EP3 0.3 nM (Ki) |
EP4 916 nM (Ki) |
EP1 >5000 nM (Ki) |
EP2 >5000 nM (Ki) |
体外実験
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).
体内実験
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.
化学情報
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CAS 番号 244101-02-8
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性状 Solid
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分子量 536.44
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分子式 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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別名
CM9; GW671021
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-15274 関連分類
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