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• 产品描述： Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively

• 靶点： IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells);SGLT

• 体外研究：
  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

• 体内研究：
  Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice. 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. Animal Model: Diet-induced obese, insulin resistantmice (DIO) Mice Dosage: 30 mg/kg Administration: Oral gavage; daily; 4 weeks Result: Reduced BG levels, respiratory exchange ratio, and body weight gain. Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats Dosage: 3 mg/kg Administration: Oral gavage; daily; 3 weeks Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.

• 参考文献：
  1. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.205 ml	11.025 ml	22.05 ml
  5 mM	0.441 ml	2.205 ml	4.41 ml
  10 mM	0.22 ml	1.102 ml	2.205 ml
  50 mM	0.044 ml	0.22 ml	0.441 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *