store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Canagliflozin hemihydrate (TA 7284) (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂,作用于表达 mSGLT2,rSGLT2 和 hSGLT2 的 CHO 细胞,IC50 分别为 2 nM,3.7 nM 和 4.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 399 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 413 | 现货 |
产品描述 | Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories. |
靶点活性 | mSGLT2/rSGLT2/hSGLT2 (CHOK cells):2/3.7/4.4 nM (IC50) |
体外活性 | Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1]. |
体内活性 | Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice[1]. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats[1]. |
别名 | JNJ28431754, TA 7284, TA7284, TA-7284, JNJ 28431754, JNJ-28431754 |
分子量 | 907.05 |
分子式 | C48H52F2O11S2 |
CAS No. | 928672-86-0 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90mg/mL (198.4mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.1025 mL | 5.5124 mL | 11.0248 mL | 27.5619 mL |
5 mM | 0.2205 mL | 1.1025 mL | 2.205 mL | 5.5124 mL | |
10 mM | 0.1102 mL | 0.5512 mL | 1.1025 mL | 2.7562 mL | |
20 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3781 mL | |
50 mM | 0.022 mL | 0.1102 mL | 0.2205 mL | 0.5512 mL | |
100 mM | 0.011 mL | 0.0551 mL | 0.1102 mL | 0.2756 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Canagliflozin hemihydrate 928672-86-0 GPCR/G Protein SGLT Canagliflozin JNJ28431754 TA 7284 TA7284 TA-7284 JNJ 28431754 JNJ-28431754 Canagliflozin Hemihydrate Inhibitor inhibitor inhibit