GR 113808
Based on 9 publication(s) in Google Scholar
GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
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: 99.68%
- CAS 番号: 144625-51-4
- 分子式: C19H27N3O4S
- 分子量:393.50
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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MedChemExpress（MCE）の使用を引用している文献 GR 113808
More- Int J Biol Sci. 2024 Aug 19;20(11):4476-4495. [Abstract]
- Phytomedicine. 2026 Jun:155:158088. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Inflamm Res. 2024 Nov 19:17:8945-8964. [Abstract]
- Transl Pediatr. 2025 Jun 27;14(6):1213-1229. [Abstract]
- Curr Med Sci. 2025 Aug 29. [Abstract]
- SSRN. 2025 Aug 7.
- SSRN. 2025 Apr 24.
5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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5-HT1B Receptor |
5-HT4 Receptor |
5-HT1A Receptor |
5-HT3 Receptor |
5-HT2A Receptor |
5-HT2C Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.21 nM
Compound: 5
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Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
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[PMID: 23043420] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:1 mg/Kg
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Administration:Intraperitoneal injection; 1 mg/Kg; 5-7 days starting 24 h after induction of colitis
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Result:Blocked protective effects of tegaserod after induction of colitis.
化学情報
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CAS 番号 144625-51-4
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性状 Solid
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分子量 393.50
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分子式 C19H27N3O4S
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Color White to off-white
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SMILES
O=C(C1=CN(C)C2=C1C=CC=C2)OCC3CCN(CCNS(=O)(C)=O)CC3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
Chronic Stress-induced Serotonin Impairs Intestinal Epithelial Cell Mitochondrial Biogenesis via the AMPK-PGC-1α Axis. [Abstract]2024 Aug 19;20(11):4476-4495. PMID: 39247815 -
Phytomedicine
Si-Ni-San alleviates depressive-like behaviors in adolescent male mice by restoring DRN-NAc serotonergic circuit function and 5-HT4R-dependent synaptic plasticity. [Abstract]2026 Jun:155:158088. PMID: 41886949 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
J Inflamm Res
Early-Life Stress Induced by Neonatal Maternal Separation Leads to Intestinal 5-HT Accumulation and Causes Intestinal Dysfunction. [Abstract]2024 Nov 19:17:8945-8964. PMID: 39588137 -
Transl Pediatr
Chenodeoxycholic acid activates the TGR5/TRPA1-5-HT pathway to regulate intestinal motility in breastfed infants and mouse models. [Abstract]2025 Jun 27;14(6):1213-1229. PMID: 40688229 -
Curr Med Sci
Konjac Oligosaccharide Alleviates Constipation in Mice via 5-HT4R/cAMP/PKA/p-CREB Pathway Activation. [Abstract]2025 Aug 29. PMID: 40879997 -
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溶剤 & 溶解度
DMSO : 39 mg/mL (99.11 mM; Need ultrasonic and warming; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (275 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)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gale JD, et al. GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.Br J Pharmacol. 1994 Jan;111(1):332-8. [Content Brief]
[2]. Spohn SN, et al.Protective Actions of Epithelial 5-Hydroxytryptamine 4 Receptors in Normal and Inflamed Colon.Gastroenterology. 2016 Nov;151(5):933-944.e3. [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 (sealed storage, away from moisture). 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 | 2.5413 mL | 12.7065 mL | 25.4130 mL | 63.5324 mL |
| 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL | 12.7065 mL | |
| 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 mL | 6.3532 mL | |
| 15 mM | 0.1694 mL | 0.8471 mL | 1.6942 mL | 4.2355 mL | |
| 20 mM | 0.1271 mL | 0.6353 mL | 1.2706 mL | 3.1766 mL | |
| 25 mM | 0.1017 mL | 0.5083 mL | 1.0165 mL | 2.5413 mL | |
| 30 mM | 0.0847 mL | 0.4235 mL | 0.8471 mL | 2.1177 mL | |
| 40 mM | 0.0635 mL | 0.3177 mL | 0.6353 mL | 1.5883 mL | |
| 50 mM | 0.0508 mL | 0.2541 mL | 0.5083 mL | 1.2706 mL | |
| 60 mM | 0.0424 mL | 0.2118 mL | 0.4235 mL | 1.0589 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3177 mL | 0.7942 mL |
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