Canagliflozin NEW
| Price | $43 | $61 | $97 |
| Package | 5mg | 10mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-05 |
Product Details
| Product Name: Canagliflozin | CAS No.: 842133-18-0 |
| Purity: 99.76% | Supply Ability: 10g |
| Release date: 2024/11/05 |
Product Introduction
Bioactivity
| 名稱 | Canagliflozin |
| 描述 | 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). |
| 細胞實驗 | 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) |
| 體外活性 | 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] |
| 體內活性 | 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] |
| 存儲條件 | 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. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 50 mg/mL (112.48 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 關鍵字 | Sodium-dependent glucose cotransporters | TA-7284 | JNJ-28431754 | Canagliflozin | Inhibitor | inhibit | JNJ28431754 | TA7284 | SGLT |
| 相關產品 | Dapagliflozin ((2S)-1,2-propanediol, hydrate) | Ertugliflozin L-pyroglutamic acid | Dapagliflozin | Ipragliflozin | Phlorizin | Empagliflozin | Ertugliflozin |
| 相關庫 | 經典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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