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Bexagliflozin (EGT1442) 是一种选择性的,口服有效的钠葡萄糖协同转运蛋白-2 (SGLT2) 抑制剂,对人 SGLT2 和 SGLT1 作用的 IC50值分别为 2 nM 和 5.6 μM。EGT1442在 2 型糖尿病中有研究价值。
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Bexagliflozin (EGT1442) 是一种选择性的,口服有效的钠葡萄糖协同转运蛋白-2 (SGLT2) 抑制剂,对人 SGLT2 和 SGLT1 作用的 IC50值分别为 2 nM 和 5.6 μM。EGT1442在 2 型糖尿病中有研究价值。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 477 | 现货 | |
2 mg | ¥ 690 | 现货 | |
5 mg | ¥ 987 | 现货 | |
10 mg | ¥ 1,580 | 现货 | |
25 mg | ¥ 3,380 | 现货 | |
50 mg | ¥ 4,920 | 现货 | |
100 mg | ¥ 6,880 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,110 | 现货 |
产品描述 | Bexagliflozin (EGT1442) is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 5.6 μM and 2 nM for human SGLT1 and SGLT2, respectively |
体内活性 | EGT1442在大鼠和犬的稳定尿糖排泄方面表现出有效性,其ED50值分别为0.38 mg/kg和0.09 mg/kg,并且在db/db小鼠中以浓度依赖的方式降低HbA(1c)和血糖水平。 |
动物实验 | Prior to experiment initiation, 7-week old SHRSP rats were assigned to 3 groups of 15 males each, based on body weights. During this week, daily water consumption was determined in order to calculate appropriate drug concentrations for the drinking water. The following week (Day 1), rats were switched to a stroke-promoting diet containing reduced potassium and protein and elevated NaCl. Animals received water bottles containing either no compound, EGT1442 (3.0 mg/kg) or the sodium channel blocker amiloride (1.0 mg/kg). Body weights were measured 2 times per week, and dosages were adjusted weekly. Water consumption was likewise measured 2 times per week, while food consumption wasmeasured weekly. Daily values were estimated. Urine samples were analyzed by test strips once every two weeks. Additionally, all animals were observed twice daily and any abnormal findings were recorded. |
别名 | THR-1442, EGT1442, EGT0001442 |
分子量 | 464.94 |
分子式 | C24H29ClO7 |
CAS No. | 1118567-05-7 |
Smiles | OC[C@H]1O[C@H]([C@H](O)[C@@H](O)[C@@H]1O)c1ccc(Cl)c(Cc2ccc(OCCOC3CC3)cc2)c1 |
密度 | 1.41 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 100 mg/mL (215.08 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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