产品说明书
Canagliflozin
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同义名 : | JNJ 28431754;TA-7284;JNJ-24831754 |
| CAS号 : | 842133-18-0 | |
| 货号 : | A335983 | |
| 分子式 : | C24H25FO5S | |
| 纯度 : | 95% | |
| 分子量 : | 444.52 | |
| MDL号 : | MFCD18251436 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(112.48 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
0.5% CMC+0.25% Tween 80+water 18 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Sodium glucose co-transporter 2 (SGLT2) is a high-capacity glucose transporter mediating the majority of the glucose resorption in kidney. Canagliflozin is a selective, potent SGLT2 inhibitor with IC50 values of 4.4, 3.7, and 2.0 nM for human SGLT2, rat SGLT2, and mouse SGLT2, respectively. In contrast, canagliflozin inhibited human, rat and mouse SGLT1 with IC50 values of 684, 571, and >1000 nM, respectively. In L6 myoblasts, canagliflozin at 10 μM blocked the non-Na+-linked GLUT-mediated 3H-2-DG uptake by < 50%. Canagliflozin at 10 μM inhibited DNJ-induced currents by 23.4% in SGLT3-injected oocytes, whereas the same treatment of canagliflozin had no effect on currents in water-injected oocytes. In Zucker diabetic fatty (ZDF) rats treated by 1 mg/kg canagliflozin hemihydrate, renal threshold for glucose excretion was reduced from 415 mg/dl to 94 mg/dl at 90 min post treatment. In db/db mice, single dose of canagliflozin (1 and 10 mg/kg) rapidly downregulated non-fasting blood glucose concentration in a dose-dependent manner at 1h post treatment. When ZDF rats were treated with canagliflozin at different doses (3, 10, or 30 mg/kg) for 4 weeks, the non-fasting blood glucose and the level of HbA1c were decreased in all canagliflozin hemihydrate-treated rats compared to control group. Decreased blood glucose level following an oral glucose tolerance test was also observed in canagliflozin hemihydrate-treated rats. Treatment of 30 mg/kg canagliflozin in DIO mice for 4 weeks decreased their blood glucose level, respiratory exchange ratio, and body weight gain compared to vehicle-treated mice[2]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CHO-K1 cells | Function assay | Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay, IC50=6.7 nM | 22652255 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02053116 | Type 2 Diabetes Mellitus | Phase 2 | Terminated(On 25April2014, stu... 展开 >>dy was terminated before any dosing due to an AE of safety concern that occurred in protocol B1731003 with the same drug.) 收起 << | - | United States, Florida ... 展开 >> Pfizer Investigational Site DeLand, Florida, United States, 32720 收起 << |
| NCT00650806 | - | Completed | - | - | |
| NCT01273558 | Diabetes Mellitus, Type 2 | Phase 1 | Completed | - | Germany ... 展开 >> Neuss, Germany 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.22mL |
11.25mL 2.25mL 1.12mL |
22.50mL 4.50mL 2.25mL |
