Tamanho : 1mLx10mM(inDMSO)
Synonyms: TA 7284, JNJ 28431754AAA, JNJ 28431754, JNJ 24831754ZAE
| 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 | 14C-AMG uptake:684 ± 159 nM (CHO-hSGLT1 cells), SGLT2 (human):4.4 nM, SGLT2 (rat):3.7 nM, SGLT2 (mouse):2 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] |
| Synonyms | TA 7284, JNJ 28431754AAA, JNJ 28431754, JNJ 24831754ZAE |
| 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) |
| 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 Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 250 mg/mL (562.4 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), Solution. 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 | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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