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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Tofogliflozin (also known as CSG-452) hydrate is a novel, very potent and highly selective inhibitor of sodium/glucose cotransporter 2 (SGLT2) with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse respectively. Tofogliflozin competitively inhibited SGLT2 in cells that overexpress SGLT2. The selectivity of tofogliflozin towards human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 is the highest among the tested SGLT2 inhibitors under clinical trials. Long-term inhibition of renal SGLT2 by tofogliflozin not only preserved pancreatic beta-cell function, but also prevented kidney dysfunction in a mouse model of type 2 diabetes. These findings suggest that long-term use of tofogliflozin in patients with type 2 diabetes may prevent progression of diabetic nephropathy.
| ln Vitro |
When tubular cells are exposed to high glucose levels, tofofloxacin (3–30 nM) treatment for 24 hours inhibits the production of oxidative stress and the expression of the monocyte chemoattractant protein-1 (MCP-1) gene[2]. Treatment with tofofloxacin (3–30 nM; 8 days; tubular epithelial cells) prevents the high glucose-induced apoptotic cell death[2].
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| ln Vivo |
The treatment of obese diabetic mice with tofogliflozin (0.1–10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) improves hyperglycemia and, consequently, ameliorates glucose intolerance[1].
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| Cell Assay |
RT-PCR[2]
Cell Types: Tubular epithelial cells Tested Concentrations: 3 nM and 30 nM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited MCP -1 gene expression in tubular cells induced by high glucose exposure. Apoptosis Analysis[2] Cell Types: Tubular epithelial cells Tested Concentrations: 3 nM and 30 nM Incubation Duration: 8 days Experimental Results: Inhibited the apoptotic cell death induced by high glucose. |
| Animal Protocol |
Animal/Disease Models: db/db mice[1] ]
Doses: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, or 10 mg/kg Route of Administration: Oral administration; one time/day; for 4 weeks Experimental Results: Observed acute blood glucose reduction, dose-dependently decreased glycated hemoglobin, Dramatically prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight. |
| References |
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| Additional Infomation |
Tofogliflozin has been used in trials studying the treatment and prevention of Diabetes Mellitus Type 2.
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| Molecular Formula |
C22H26O6.H2O
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| Molecular Weight |
404.45
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| Exact Mass |
404.184
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| CAS # |
1201913-82-7
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| Related CAS # |
Tofogliflozin;903565-83-3
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| PubChem CID |
46908928
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| Appearance |
White to off-white solid powder
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| LogP |
0.932
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
521
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCC1=CC=C(C=C1)CC2=CC3=C(CO[C@@]34[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)C=C2.O
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| InChi Key |
ZXOCGDDVNPDRIW-NHFZGCSJSA-N
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| InChi Code |
InChI=1S/C22H26O6.H2O/c1-2-13-3-5-14(6-4-13)9-15-7-8-16-12-27-22(17(16)10-15)21(26)20(25)19(24)18(11-23)28-22;/h3-8,10,18-21,23-26H,2,9,11-12H2,1H3;1H2/t18-,19-,20+,21-,22+;/m1./s1
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| Chemical Name |
(3S,3'R,4'S,5'S,6'R)-5-[(4-ethylphenyl)methyl]-6'-(hydroxymethyl)spiro[1H-2-benzofuran-3,2'-oxane]-3',4',5'-triol;hydrate
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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. Solubility in Formulation 4: 2.5 mg/mL (6.18 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| 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.
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