| 產(chǎn)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 |
| 靶點(diǎn)： |
IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells);SGLT |
| 體外研究： |
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 |
| 體內(nèi)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. |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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 |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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