| Size | Price | Stock | Qty |
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| 50mg |
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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 (formerly TA-7284; JNJ-24831754ZAE; JNJ 28431754-AAA; JNJ-28431754; brand name Invokana) is a highly potent and selective SGLT2 (sodium-glucose transport protein) inhibitor with anti-diabetic activity. The FDA has authorized canagliflozin for the management of type 2 diabetes. In a cell-free assay, it suppresses hSGLT2 with an IC50 of 2.2 nM and demonstrates >413-fold selectivity over hSGLT1.
| Targets |
mSGLT2 ( IC50 = 2 nM ); rSGLT2 ( IC50 = 3.7 nM ); hSGLT2 ( IC50 = 4.4 nM )
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| Enzyme Assay |
Canagliflozin is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM, and exhibits 413-fold selectivity over hSGLT1.
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| Cell Assay |
The effect of canagliflozin on the activity of the glucose transporter 1 (GLUT1) is examined in rat skeletal muscle cell line L6 cells. The culture medium used for the cells is Dulbecco's modified Eagle's medium, which contains 5.6 mM glucose and 10% fetal bovine serum. The cells are seeded in 24-well plates at a density of 3 × 105 cells/well and are cultured for 24 hours at 37 °C in an atmosphere of 5% CO2. The cells are pre-incubated with the solutions of Canagliflozin (250 μL, 10 μM) for 5 minutes at room temperature after being rinsed twice with Kreb's ringer phosphate HEPES buffer (pH 7.4, 150 mM NaCl, 5 mM KCl, 1.25 mM MgSO4, 1.25 mM CaCl2, 2.9 mM Na2HPO4, 10 mM HEPES). 50 μL of 4.5 mM 2-DG (a GLUTs substrate)/3H-2-DG (0.625 μCi) is added to start the transport reaction, which is then incubated for 15 minutes at room temperature. Aspiration of the incubation mixture stops the uptake of 2-DG. The cells are instantly cleaned three times in ice-cold PBS. Radioactivity is measured using liquid scintillation after samples are extracted using 0.3 N NaOH.
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| References |
| Molecular Formula |
C24H25FO5S
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| Molecular Weight |
444.52
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| Exact Mass |
444.14
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| Elemental Analysis |
C, 64.85; H, 5.67; F, 4.27; O, 18.00; S, 7.21
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| CAS # |
842133-18-0
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| Related CAS # |
Canagliflozin hemihydrate; 928672-86-0; Canagliflozin-d4; 1997338-61-0; Canagliflozin-d6
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| Appearance |
White solid powder
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| SMILES |
CC1=C(C=C(C=C1)[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F
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| InChi Key |
XTNGUQKDFGDXSJ-ZXGKGEBGSA-N
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| InChi Code |
InChI=1S/C24H25FO5S/c1-13-2-3-15(24-23(29)22(28)21(27)19(12-26)30-24)10-16(13)11-18-8-9-20(31-18)14-4-6-17(25)7-5-14/h2-10,19,21-24,26-29H,11-12H2,1H3/t19-,21-,22+,23-,24+/m1/s1
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| Chemical Name |
(2S,3R,4R,5S,6R)-2-[3-[[5-(4-fluorophenyl)thiophen-2-yl]methyl]-4-methylphenyl]-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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2496 mL | 11.2481 mL | 22.4962 mL | |
| 5 mM | 0.4499 mL | 2.2496 mL | 4.4992 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2496 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05856578 | Active Recruiting |
Drug: Mulberry Twig Alkaloid Tablet Drug: Canagliflozin |
Type 2 Diabetes Mellitus | Nanjing First Hospital, Nanjing Medical University |
March 15, 2022 | Phase 4 |
| NCT02624908 | Active Recruiting |
Drug: canagliflozin Drug: placebo |
Diabetes Mellitus, Type 2 | Foundation for Atlanta Veterans Education and Research, Inc. |
January 2016 | Phase 4 |
| NCT05135039 | Recruiting | Drug: Canagliflozin Drug: Placebo |
PreDiabetes Hiv |
xiaolong zhao | January 1, 2022 | Not Applicable |
| NCT05364190 | Recruiting | Drug: Canagliflozin Drug: Empagliflozin |
Chronic Heart Failure Acute Heart Failure |
October 6 University | June 4, 2022 | Phase 3 |
| NCT05427084 | Not yet recruiting | Drug: Canagliflozin Drug: Placebo |
Diabetes Type 2 Coronary Artery Disease |
Ottawa Heart Institute Research Corporation |
December 2023 | Phase 2 Phase 3 |
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