Ipragliflozin
Based on 8 publication(s) in Google Scholar
Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.71%
- CAS No.: 761423-87-4
- Formule: C21H21FO5S
- Masse moléculaire:404.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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
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HY-10450
DapagliflozinSGLT2 Inhibitor -
HY-15409
EmpagliflozinSGLT2 Inhibitor -
HY-10451
CanagliflozinSGLT2 Inhibitor -
HY-15516
SotagliflozinSGLT Inhibitor -
HY-15461
ErtugliflozinSGLT2 Inhibitor -
HY-13413
Tofogliflozin hydrateSGLT2 Inhibitor -
HY-N0143
PhlorizinSGLT Inhibitor -
HY-I0383
Canagliflozin hemihydrateSGLT Inhibitor -
HY-10450R
Dapagliflozin (Standard)SGLT2 Inhibitor -
HY-N0142
PhloretinAnti-inflammatory Agent -
HY-15409R
Empagliflozin (Standard)SGLT2 Inhibitor -
HY-14894R
Ipragliflozin (Standard)SGLT Inhibitor
Publications Citing Use of MedChemExpress (MCE) Ipragliflozin
More- Int J Biol Macromol. 2024 Dec;282(Pt 3):137003. [Abstract]
- Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]
- Biochem Pharmacol. 2016 Feb 1:101:27-39. [Abstract]
- Hypertens Res. 2017 Jul;40(7):646-651. [Abstract]
- Int J Med Sci. 2018 Jun 13;15(9):937-943. [Abstract]
- Mol Carcinog. 2025 Jan;64(1):192-208. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Sep 1:1000:22-8. [Abstract]
- University of Paris. 2022 Sep 19.
Activité biologique
Description
IC50 & Target
[1]|
hSGLT2 7.38 nM (IC50) |
hSGLT1 1876 nM (IC50) |
rSGLT2 6.73 nM (IC50) |
rSGLT1 1166 nM (IC50) |
mSGLT2 5.64 nM (IC50) |
mSGLT1 1380 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
7.4 nM
Compound: 14h, ASP1941, ipragliflozin
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Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting
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[PMID: 22507206] |
In Vitro
Ipragliflozin (1-50 μM) significantly and dose-dependently suppresses the growth of MCF-7 human breast cancer cell lines.
Upon knocking down SGLT2 expression using siRNA, the attenuation of cell proliferation induced by Ipragliflozin is completely canceled, suggesting that Ipragliflozin attenuates breast cancer cell proliferation through SGLT2 inhibition.
BrdU assay revealed that Ipragliflozin at a high dose (50 and 100 μM) significantly inhibits DNA synthesis of MCF-7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:MCF-7 human breast cancer cell lines
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Concentration:1, 10, 50 μM
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Incubation Time:24, 48, 72, 96 hours
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Result:Decreased the number of MCF-7 cells in a dose-dependent manner.
In Vivo
Ipragliflozin (0.3 and 1 mg/kg) shows antidiabetic effects of repeated administration in streptozotocin-induced type 1 diabetic rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Single Administration[1]
Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice -
Dosage:0.1-1 mg/kg
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Administration:Single oral administration in the fed condition. Blood glucose levels were then measured for 8 h under fasting conditions.
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Result:Dose-dependently lowered blood glucose levels, and this effect was significant at all tested doses.
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Animal Model:Repeated Administration[1]
Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats -
Dosage:0.3 and 1 mg/kg
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Administration:Administration orally once daily (at night) for 4 weeks.
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Result:Significantly reduced the levels of HbA1c and blood glucose. Pancreatic insulin content was significantly increased at a dose of 1 mg/kg. Urinary glucose excretion was increased dose-dependently, and this was significant at the 1 mg/kg dose.
Chemical Information
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CAS No. 761423-87-4
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Appearance Solid
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Masse moléculaire 404.45
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Formule C21H21FO5S
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Color White to off-white
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SMILES
FC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)C=C1CC3=CC(C=CC=C4)=C4S3
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Synonyms
ASP1941
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Drug repurposing: An antidiabetic drug Ipragliflozin as Mycobacterium tuberculosis sirtuin-like protein inhibitor that synergizes with anti-tuberculosis drug isoniazid. [Abstract]2024 Dec;282(Pt 3):137003. PMID: 39481722 -
Biochem Pharmacol
Canagliflozin exerts anti-inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells. [Abstract]2018 Jun:152:45-59. PMID: 29551587 -
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Hypertens Res
Arterial pressure lability is improved by sodium-glucose cotransporter 2 inhibitor in streptozotocin-induced diabetic rats. [Abstract]2017 Jul;40(7):646-651. PMID: 28202943 -
Int J Med Sci
Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. [Abstract]2018 Jun 13;15(9):937-943. PMID: 30008607 -
Mol Carcinog
ZNF480 Accelerates Chemotherapy Resistance in Breast Cancer by Competing With TRIM28 and Stabilizing LSD1 to Upregulate the AKT-GSK3β-Snail Pathway. [Abstract]2025 Jan;64(1):192-208. PMID: 39503216 -
J Chromatogr B Analyt Technol Biomed Life Sci
A quantitative LC-MS/MS method for determining ipragliflozin, a sodium-glucose co-transporter 2 (SGLT-2) inhibitor, and its application to a pharmacokinetic study in rats. [Abstract]2015 Sep 1:1000:22-8. PMID: 26209767 -
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (247.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (6.18 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 (6.18 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.
In Vivo Dissolution Calculator
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.
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 (283 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Atsuo Tahara, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36. [Content Brief]
[2]. Shiho Komatsu, et al. SGLT2 inhibitor ipragliflozin attenuates breast cancer cell proliferation. Endocr J. 2020 Jan 28;67(1):99-106. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4725 mL | 12.3625 mL | 24.7249 mL | 61.8123 mL |
| 5 mM | 0.4945 mL | 2.4725 mL | 4.9450 mL | 12.3625 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4725 mL | 6.1812 mL | |
| 15 mM | 0.1648 mL | 0.8242 mL | 1.6483 mL | 4.1208 mL | |
| 20 mM | 0.1236 mL | 0.6181 mL | 1.2362 mL | 3.0906 mL | |
| 25 mM | 0.0989 mL | 0.4945 mL | 0.9890 mL | 2.4725 mL | |
| 30 mM | 0.0824 mL | 0.4121 mL | 0.8242 mL | 2.0604 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 50 mM | 0.0494 mL | 0.2472 mL | 0.4945 mL | 1.2362 mL | |
| 60 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL | 1.0302 mL | |
| 80 mM | 0.0309 mL | 0.1545 mL | 0.3091 mL | 0.7727 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2472 mL | 0.6181 mL |
Ipragliflozin Related Classifications
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