生物活性
canagliflozin是2型亚钠葡萄糖转运蛋白（SGLT2）的抑制剂,作用于hSGLT2，无细胞试验中IC50为2.2 nM，比作用于hSGLT1选择性高413倍。
靶点信息
| mSGLT2 (Cell-free assay) | rSGLT2 (Cell-free assay) | hSGLT2 (Cell-free assay) | | |
| 2 nM | 3.7 nM | 4.4 nM | | |
化学数据
| 目录号 | A11100 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 444.5 |
| Formula | C24H25FO5S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 842133-18-0 |
| SMILES | CC1=C(C=C(C=C1)[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F |
溶解度
| In vitro (25°C) | DMSO | 79 mg/mL (177.71 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 0.5% CMC+0.25% Tween 80 | 17 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 22.5 mL | 112.49 mL | 224.97 mL |
| 0.5 mM | 4.5 mL | 22.5 mL | 44.99 mL |
| 1 mM | 2.25 mL | 11.25 mL | 22.5 mL |
| 5 mM | 0.45 mL | 2.25 mL | 4.5 mL |
*The above data is based on the productmolecular weight 444.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
