Remogliflozin etabonate
Based on 1 Customer Validation
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 442201-24-3
- Formula: C26H38N2O9
- Molecular Weight:522.59
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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hSGLT2 1.95 μM (Ki) |
rSGLT2 2.14 μM (Ki) |
hSGLT1 43.1 μM (Ki) |
rSGLT1 8.57 μM (Ki) |
Remogliflozin etabonate (3, 10, 30 mg/kg; orally) increases urinary glucose excretion in a dose-dependent manner. Remogliflozin etabonate dose-dependently inhibits the increase in plasma glucose after glucose loading and decreases the plasma insulin in normal rats[1].
Remogliflozin etabonate (1-10 mg/kg; orally) decreases the blood glucose and reduces the AUC0–6 h for blood glucose in a dose-dependent manner[1].
Remogliflozin etabonate (high-fat diet containing 0.01, 0.03, or 0.1% remogliflozin etabonate for 8 weeks) reduces the levels of plasma glucose, plasma insulin, and GHb in a dose-dependent manner, and it suppresses the development of hypertriglyceridemia in male GK rats (6 weeks of age)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db mice at the age of 8 weeks[1]
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Dosage:10 or 30 mg/kg
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Administration:Orally; twice daily for 6 weeks
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Result:Significantly reduced both the fasting plasma glucose (FPG) and glycated hemoglobin (GHb) levels in a dosedependent manner.
Reduced both urine volume and urinary glucose excretion with ameliorated the hyperglycemia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 442201-24-3
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Appearance Solid
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Molecular Weight 522.59
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Formula C26H38N2O9
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Color White to off-white
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SMILES
CCOC(OC[C@H]1O[C@H]([C@@H]([C@@H](O)[C@@H]1O)O)OC2=NN(C(C)C)C(C)=C2CC3=CC=C(OC(C)C)C=C3)=O
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Synonyms
GSK189075
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (191.35 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 (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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.78 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 (4.78 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.
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.
Purity & Documentation
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Data Sheet (278 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)
References
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 | 1.9135 mL | 9.5677 mL | 19.1355 mL | 47.8386 mL |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.8271 mL | 9.5677 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9135 mL | 4.7839 mL | |
| 15 mM | 0.1276 mL | 0.6378 mL | 1.2757 mL | 3.1892 mL | |
| 20 mM | 0.0957 mL | 0.4784 mL | 0.9568 mL | 2.3919 mL | |
| 25 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9135 mL | |
| 30 mM | 0.0638 mL | 0.3189 mL | 0.6378 mL | 1.5946 mL | |
| 40 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1960 mL | |
| 50 mM | 0.0383 mL | 0.1914 mL | 0.3827 mL | 0.9568 mL | |
| 60 mM | 0.0319 mL | 0.1595 mL | 0.3189 mL | 0.7973 mL | |
| 80 mM | 0.0239 mL | 0.1196 mL | 0.2392 mL | 0.5980 mL | |
| 100 mM | 0.0191 mL | 0.0957 mL | 0.1914 mL | 0.4784 mL |
Remogliflozin etabonate Related Classifications
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