Luseogliflozin
Based on 1 publication(s) in Google Scholar
Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC50 of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC50, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes.
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- Pureté: 99.33%
- CAS No.: 898537-18-3
- Formule: C23H30O6S
- Masse moléculaire:434.55
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Luseogliflozin
More
Activité biologique
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SGLT2 2.26 nM (IC50) |
SGLT1 3990 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
2.26 nM
Compound: 3p
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Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake
Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of glucose uptake
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[PMID: 20302302] |
| CHO-K1 | IC50 |
3990 nM
Compound: 3p
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Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of glucose uptake
Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of glucose uptake
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[PMID: 20302302] |
Luseogliflozin competitively inhibits the sodium-dependent uptake of 14C-α-methylglucoside by Chinese hamster ovary K1 cells overexpressing human SGLT2 in vitro (Ki value 1.10 nM)[1].
Luseogliflozin (20% OSI-096 (HY-10191) and Luseogliflozin-generated serum, 24 h) induces β-cell proliferation through a humoral factor-mediated FoxM1/PLK1/CENP-A pathway independent of insulin signaling[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:β cell
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Concentration:20% OSI-096 and Luseogliflozin-generated serum
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Incubation Time:24 h
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Result:Promoted β-cell proliferation and significantly increased gene expression levels of Foxm1, Cenpa, Plk1 and Ccnb1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J male mice induced by OSI-906[2]
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Dosage:10 mg/kg/daily, 7 days
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Administration:Oral
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Result:Inhibited SGLT2 and significantly improved hyperglycemia in mice, but did not improve hyperinsulinemia.Had no effect on hepatic steatosis and adipose tissue atrophy, and improved the quality and proliferation of β cells.
Chemical Information
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CAS No. 898537-18-3
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Appearance Solid
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Masse moléculaire 434.55
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Formule C23H30O6S
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Color White to off-white
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SMILES
OC[C@@H](S1)[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1C2=C(OC)C=C(C)C(CC3=CC=C(OCC)C=C3)=C2
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Synonyms
TS 071
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 25 mg/mL (57.53 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 (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.
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.
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: ≥ 1.25 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 (protect from light)
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Anthony Markham,et al. Luseogliflozin: first global approval. Drugs. 2014 Jun;74(8):945-50. [Content Brief]
[2]. Jun Shirakawa,et al. Luseogliflozin increases beta cell proliferation through humoral factors that activate an insulin receptor- and IGF-1 receptor-independent pathway. Diabetologia. 2020 Mar;63(3):577-587. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3012 mL | 11.5062 mL | 23.0123 mL | 57.5308 mL |
| 5 mM | 0.4602 mL | 2.3012 mL | 4.6025 mL | 11.5062 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3012 mL | 5.7531 mL | |
| 15 mM | 0.1534 mL | 0.7671 mL | 1.5342 mL | 3.8354 mL | |
| 20 mM | 0.1151 mL | 0.5753 mL | 1.1506 mL | 2.8765 mL | |
| 25 mM | 0.0920 mL | 0.4602 mL | 0.9205 mL | 2.3012 mL | |
| 30 mM | 0.0767 mL | 0.3835 mL | 0.7671 mL | 1.9177 mL | |
| 40 mM | 0.0575 mL | 0.2877 mL | 0.5753 mL | 1.4383 mL | |
| 50 mM | 0.0460 mL | 0.2301 mL | 0.4602 mL | 1.1506 mL |
Luseogliflozin Related Classifications
HY-10449 Related Classifications
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