Mizagliflozin
Based on 5 publication(s) in Google Scholar
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
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- Reinheit: 99.20%
- CAS. Nr.: 666843-10-3
- Formel: C28H44N4O8
- Molecular Weight:564.67
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Mizagliflozin
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Biologische Aktivität
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SGLT1 |
Mizagliflozin administrated intravenously (0.3 mg/kg) and orally (3 mg/kg) declined with a short half-life (0.23 and 1.14 h, respectively)[2]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (rat model of low-fiber-diet-induced constipation)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:Oral
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Result:Increased fecal wet weight in a rat model of low-fiber-diet-induced constipation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 666843-10-3
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Appearance Solid
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Molecular Weight 564.67
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Formel C28H44N4O8
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Color Off-white to light yellow
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SMILES
O=C(N)C(C)(C)CNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C(C)=C1
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Synonyms
DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
2025 Aug;644(8078):1069-1077. PMID: 40634617 -
Nat Biomed Eng
Glucosylated nanoparticles for the oral delivery of antibiotics to the proximal small intestine protect mice from gut dysbiosis. [Abstract]2022 Jul;6(7):867-881. PMID: 35798834 -
Basic Res Cardiol
SGLT1 contributes to glucose-mediated exacerbation of ischemia-reperfusion injury in ex vivo rat heart. [Abstract]2024 Oct;119(5):733-749. PMID: 39088085 -
RSC Adv
Synthesis, radiolabeling, and biological evaluation of methyl 6-deoxy-6-[18F]fluoro-4-thio-α-d-maltotrioside as a positron emission tomography bacterial imaging agent. [Abstract]2025 Mar 21;15(11):8809-8829. PMID: 40124918 -
Lösungsmittel & Löslichkeit
H2O : ≥ 100 mg/mL (177.09 mM)
DMSO : 100 mg/mL (177.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.43 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.43 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (277 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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Handling Instructions (2659 KB)
Verweise
[1]. Inoue T, et al. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur J Pharmacol. 2017 Jul 5;806:25-31. [Content Brief]
[2]. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.7709 mL | 8.8547 mL | 17.7095 mL | 44.2736 mL |
| 5 mM | 0.3542 mL | 1.7709 mL | 3.5419 mL | 8.8547 mL | |
| 10 mM | 0.1771 mL | 0.8855 mL | 1.7709 mL | 4.4274 mL | |
| 15 mM | 0.1181 mL | 0.5903 mL | 1.1806 mL | 2.9516 mL | |
| 20 mM | 0.0885 mL | 0.4427 mL | 0.8855 mL | 2.2137 mL | |
| 25 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7709 mL | |
| 30 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 40 mM | 0.0443 mL | 0.2214 mL | 0.4427 mL | 1.1068 mL | |
| 50 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL | |
| 60 mM | 0.0295 mL | 0.1476 mL | 0.2952 mL | 0.7379 mL | |
| 80 mM | 0.0221 mL | 0.1107 mL | 0.2214 mL | 0.5534 mL | |
| 100 mM | 0.0177 mL | 0.0885 mL | 0.1771 mL | 0.4427 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Mizagliflozin Related Classifications
HY-17638 Related Classifications
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