| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Canagliflozin hemihydrate (also known as TA-7284; JNJ-24831754ZAE; JNJ 28431754AAA; JNJ-28431754; Invokana), the hemihydrated form of Canagliflozin, is a highly potent and selective SGLT2 inhibitor with anti-diabetic effects. It inhibits hSGLT2 with IC50 of 2.2 nM in a cell-free assay. Canagliflozin exhibits 413-fold selectivity over hSGLT1. Canagliflozin is a FDA approved drug for the treatment of type 2 diabetes. Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Canagliflozin was approved by the FDA on March 29, 2013, and became the first SGLT2 inhibitor approved in the USA.
| ln Vitro |
In CHO-hSGLT2 cells, canagliflozin inhibits Na+-dependent 14C-AMG uptake with an IC50 of 4.4±1.2 nM. Rat and mouse SGLT2 have IC50 values of 2.0 nM and 3.7 nM, respectively, in CHO-mSGLT2 and CHO-rSGLT2 cells. With an IC50 of 684±159 nM and >1,000 nM, respectively, canagliflozin inhibits the absorption of 14C-AMG in CHO-hSGLT1 and mSGLT1 cells[1].
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| ln Vivo |
In DIO mice, canagliflozin (30 mg/kg) therapy for 4 weeks lowers body weight increase, respiratory exchange ratio, and blood glucose (BG) levels[1]. as canagliflozin (3 mg/kg) is administered for three weeks, rats treated with ZF experience a loss in body weight due to an increase in urine glucose excretion (UGE) without a significant change in total food consumption as compared to vehicle-treated rats[1].
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| Animal Protocol |
Animal/Disease Models: Diet-induced obese, insulin resistantmice (DIO) Mice[1]
Doses: 30 mg/kg Route of Administration: po (oral gavage); daily; 4 weeks Experimental Results: decreased BG levels, respiratory exchange ratio, and body weight gain. Animal/Disease Models: Male Zucker fatty (ZF) obese, insulin resistant rats[1] Doses: 3 mg /kg Route of Administration: po (oral gavage); daily; 3 weeks Experimental Results: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight. |
| References |
[1]. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555.
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| Molecular Formula |
C48H52F2O11S2
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| Molecular Weight |
907.05
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| CAS # |
928672-86-0
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| Related CAS # |
Canagliflozin;842133-18-0
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| SMILES |
S1C(C2C([H])=C([H])C(=C([H])C=2[H])F)=C([H])C([H])=C1C([H])([H])C1=C(C([H])([H])[H])C([H])=C([H])C(=C1[H])[C@@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])O[H]
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| Synonyms |
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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 (5.51 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 (5.51 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 (5.51 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: 0.5% CMC+0.25% Tween 80 :18 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1025 mL | 5.5124 mL | 11.0248 mL | |
| 5 mM | 0.2205 mL | 1.1025 mL | 2.2050 mL | |
| 10 mM | 0.1102 mL | 0.5512 mL | 1.1025 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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