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Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2/3.7/4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $61 | In Stock | |
50 mg | $97 | In Stock | |
100 mg | $125 | In Stock | |
200 mg | $185 | In Stock | |
500 mg | $313 | In Stock | |
1 mL x 10 mM (in DMSO) | $48 | In Stock |
Description | Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2/3.7/4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM). |
Targets&IC50 | SGLT2 (human):4.4 nM, SGLT2 (mouse):2 nM, SGLT2 (rat):3.7 nM |
In vitro | METHODS: CHOK-hSGLT1 and CHOK-hSGLT2 cells were incubated with Canagliflozin (0.01-10000 nM) for 10 min and sodium-dependent glucose uptake was detected. RESULTS: Canagliflozin inhibited 14C-AMG uptake in CHO-hSGLT1 and CHOK-hSGLT2 cells with IC50 of 684±159 nM and 4.4±1.2 nM, respectively.[1] METHODS: Human umbilical vein endothelial cell HUVECs were treated with Canagliflozin (1-50 µM) for 24 h and DNA synthesis was measured to monitor cell proliferation. RESULTS: Treatment of HUVECs with Canagliflozin resulted in a concentration-dependent inhibition of DNA synthesis. The ability of Canagliflozin to block DNA synthesis was observed at concentrations (5-10 µM) achieved in the plasma of patients receiving Canagliflozin. In addition, higher concentrations of Canagliflozin (50 µM) virtually eliminated DNA synthesis. [2] |
In vivo | METHODS: To study the efficacy of treatment of type 2 diabetes mellitus (T2DM), Canagliflozin (0.1-30 mg/kg, 0.5% hydroxypropyl methylcellulose) was administered by gavage to four animal models. The animal models included: (1) male C57BL/6J mice fed a high-fat diet; (2) male C57BL/ksj-db/db hyperglycemic mice; (3) male Zucker fatty (ZF) obese, insulin-resistant rats; and (4) male ZDF obese, hyperglycemic rats. RESULTS: Canagliflozin decreased RTG and increased UGE, improved glycemic control and β-cell function, and reduced body weight gain in a rodent model of T2DM. [1] |
Cell Research | Cells from the rat skeletal muscle cell line, L6, is used to test the effect of Canagliflozin on glucose transporter 1 (GLUT1) activity. Cells are maintained in Dulbecco's modified Eagle's medium containing 5.6 mM glucose supplemented with 10% fetal bovine serum, are seeded in 24-well plates at a density of 3 × 105 cells/well and cultured for 24 hours in an atmosphere of 5% CO2 at 37 °C. Cells are 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) and are pre-incubated with the solutions of Canagliflozin (250 μL, 10 μM) for 5 minutes at room temperature. The transport reaction is initiated by adding 50 μL of 4.5 mM 2-DG (a substrate for GLUTs)/3H-2-DG (0.625 μCi) followed by incubation for 15 minutes at room temperature. The 2-DG uptake is halted by aspiration of the incubation mixture. Cells are immediately washed 3 times with ice-cold PBS. Samples are extracted with 0.3 N NaOH, and radioactivity is determined by liquid scintillation.(Only for Reference) |
Alias | TA 7284, JNJ 28431754AAA, JNJ 28431754, JNJ 24831754ZAE |
Molecular Weight | 444.52 |
Formula | C24H25FO5S |
Cas No. | 842133-18-0 |
Smiles | O[C@H]1[C@@H](O[C@H](CO)[C@@H](O)[C@@H]1O)C2=CC(CC=3SC(=CC3)C4=CC=C(F)C=C4)=C(C)C=C2 |
Relative Density. | 1.364 g/cm3 |
Storage | keep away from direct sunlight,keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (112.48 mM), Sonication is recommended. ![]() Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (11.25 mM), In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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