Dolcanatide
Based on 1 Customer Validation
Dolcanatide is an orally active GC-C (guanylate cyclase-C) agonist. Dolcanatide shows laxative, anti-nociceptive and anti-inflammatory activity. Dolcanatide can be used in inflammatory bowel disease research.
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: 99.20%
- CAS 番号: 1092457-65-2
- 分子式: C65H104N18O26S4
- 分子量:1681.89
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保管条件:
Stored under nitrogen, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
生物活性
Dolcanatide (0-10 μM; 30 min) activates GC-C receptors to stimulate cGMP synthesis in a dose-dependent manner in T84 cells[2].
Dolcanatide (1 μM; 16 h) suppresses lipopolysaccharide-induced paracellular permeability in Caco-2 and T84 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T84 cells
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Concentration:0-10 μM
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Incubation Time:30 min
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Result:Showed EC50 value of 0.28 μM.
Dolcanatide (oral administration; 0.01 and 0.05 mg/kg; once) alleviates stress-induced colorectal hypersensitivity (CRD) in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TNBS-induced rectal allodynia in rats[1]
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Dosage:0.01 and 0.05 mg/kg
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Administration:Oral administration; 0.01 and 0.05 mg/kg; once
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Result:Attenuated the TNBS-induced increase in the number of abdominal contractions (distending pressures up to 60 mmHg).
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Animal Model:Stress-induced visceral hypersensitivity in Wistar rats[1]
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Dosage:0.01 and 0.05 mg/kg
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Administration:Oral administration; 0.01 and 0.05 mg/kg; once
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Result:Resulted in a significant reduction in the rate of PRS (partial restraint stress)-induced abdominal contractions with increasing CRD (colorectal distension) pressures.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1092457-65-2
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性状 Solid
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分子量 1681.89
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分子式 C65H104N18O26S4
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Color White to off-white
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配列
{d-Asn}--Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-{d-Leu} (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
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シーケンスの短縮
{d-Asn}-DECELCVNVACTGC-{d-Leu} (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Stored under nitrogen, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
溶剤 & 溶解度
DMSO : 100 mg/mL (59.46 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 (stored under nitrogen, 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 (stored under nitrogen, 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)
純度とドキュメンテーション
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データシート (281 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]. Boulete IM, et al. Oral treatment with plecanatide or dolcanatide attenuates visceral hypersensitivity via activation of guanylate cyclase-C in rat models. World J Gastroenterol. 2018 May 7;24(17):1888-1900. [Content Brief]
[2]. Shailubhai K, et al. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis. World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):213-22. [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 (stored under nitrogen, 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 | 0.5946 mL | 2.9728 mL | 5.9457 mL | 14.8642 mL |
| 5 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | 2.9728 mL | |
| 10 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4864 mL | |
| 15 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9909 mL | |
| 20 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 25 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5946 mL | |
| 30 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL | |
| 40 mM | 0.0149 mL | 0.0743 mL | 0.1486 mL | 0.3716 mL | |
| 50 mM | 0.0119 mL | 0.0595 mL | 0.1189 mL | 0.2973 mL |