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Purity: ≥98%
Ipragliflozin (also known as ASP1941) is a novel, highly potent and selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2) with IC50 value of 7.4 nM for hSGLT2. It exhibited 254-fold selectivity for SGLT2 than SGLT1 and has little or NO activity on SGLT3/4/5/6. As a SGLT2 inhibitor, Ipragliflozin is used for the treatment of type 2 diabetes. Ipragliflozin can improve glycaemic control when used in combination with metformin. Ipragliflozin not only alleviates hyperglycemia but also improves diabetes/obesity-associated metabolic abnormalities in type 2 diabetic mice.
| ln Vitro |
In a dose-dependent manner, ipragliflozin (1-50 μM) considerably suppresses the proliferation of the human breast cancer cell line MCF-7. Ipragliflozin initially reduced breast cancer cell proliferation, but this effect was entirely eliminated when SGLT2 expression was knocked down using siRNA. This suggests that Ipragliflozin inhibits SGLT2 to minimize breast cancer cell proliferation. DNA production in MCF-7 cells was considerably decreased by high dosages (50 and 100 μM) of Ipragliflozin, as demonstrated by the BrdU assay [1].
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| ln Vivo |
Ipragliflozin exhibits hypoglycemic properties. The rise in blood glucose levels is dose-dependently inhibited by ipragliflozin (0.1–1 mg/kg). This effect was significant at doses of 0.3 and 1 mg/kg in STZ-induced type 1 diabetic rats, and significant at all tested doses in KK-Ay type 2 diabetic mice [1]. In type 1 diabetic rats induced by streptozotocin, ipragliflozin (0.3 and 1 mg/kg) demonstrated antidiabetic effects at repeated doses [1].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: MCF-7 human breast cancer cell lines Tested Concentrations: 1, 10, 50 μM Incubation Duration: 24, 48, 72, 96 hrs (hours) Experimental Results: diminished the number of MCF-7 cells in a dose- dependent manner. |
| Animal Protocol |
Animal/Disease Models: Single Administration[1] Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice
Doses: 0.1-1 mg/kg Route of Administration: Single oral administration in the fed condition. Blood glucose levels were then measured for 8 h under fasting conditions. Experimental Results: Dose-dependently lowered blood glucose levels, and this effect was significant at all tested doses. Animal/Disease Models: Repeated Administration[1] Streptozotocin (STZ; 50 mg/kg)- induced type 1 diabetic rats Doses: 0.3 and 1 mg/kg Route of Administration: Administration orally one time/day (at night) for 4 weeks. Experimental Results: Dramatically decreased the levels of HbA1c and blood glucose. Pancreatic insulin content was Dramatically 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. |
| References |
[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.
[2]. Shiho Komatsu, et al. SGLT2 inhibitor ipragliflozin attenuates breast cancer cell proliferation. Endocr J. 2020 Jan 28;67(1):99-106. |
| Additional Infomation |
Ipragliflozin is a glycoside.
Ipragliflozin is under investigation in Type 2 Diabetes and Diabetes Mellitus, Type 2. |
| Molecular Formula |
C21H21FOS
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| Molecular Weight |
404.45
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| Exact Mass |
404.109
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| CAS # |
761423-87-4
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| Related CAS # |
Ipragliflozin (L-Proline);951382-34-6
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| PubChem CID |
10453870
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
628.8±55.0 °C at 760 mmHg
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| Flash Point |
334.1±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
5.59
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
525
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| Defined Atom Stereocenter Count |
5
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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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| InChi Key |
AHFWIQIYAXSLBA-RQXATKFSSA-N
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| InChi Code |
InChI=1S/C21H21FO5S/c22-15-6-5-12(21-20(26)19(25)18(24)16(10-23)27-21)7-13(15)9-14-8-11-3-1-2-4-17(11)28-14/h1-8,16,18-21,23-26H,9-10H2/t16-,18-,19+,20-,21+/m1/s1
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| Chemical Name |
(2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4725 mL | 12.3625 mL | 24.7249 mL | |
| 5 mM | 0.4945 mL | 2.4725 mL | 4.9450 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Non-inferiority of iPragliflozin and metformin on glucose metabolism, pleiotropic effects and safety in type2 diabetes
CTID: UMIN000018979
Phase: Status: Recruiting
Date: 2015-09-11
Stability ofaipragliflozin andbphlorizin in mouse intestinal mucosal homogenates.Naunyn Schmiedebergs Arch Pharmacol.2012 Apr;385(4):423-36. |
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Effects of ipragliflozin onaurinary glucose excretion andburine volume in normal mice.Naunyn Schmiedebergs Arch Pharmacol.2012 Apr;385(4):423-36. |
Effects of ipragliflozin on blood glucose levels in streptozotocin-induced type 1 diabetic rats.Naunyn Schmiedebergs Arch Pharmacol.2012 Apr;385(4):423-36. |
Effects of ipragliflozin on blood glucose levels in KK-Aytype 2 diabetic mice.Naunyn Schmiedebergs Arch Pharmacol.2012 Apr;385(4):423-36. |
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Effects of ipragliflozin and glibenclamide on fasting blood glucose levels in normal mice.Naunyn Schmiedebergs Arch Pharmacol.2012 Apr;385(4):423-36. |
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