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。

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

EGT1442 produces a stable urinary excretion of glucose in rats and dogs with ED50 values of 0.38 and 0.09 mg/kg, respectively, and reduces HbA(1c) and blood glucose in db/db mice in a concentration dependent manner.

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.

1118567-05-7

C24H29ClO7

464.94

EGT1442;EGT0001442;THR-1442

DMSO:100 mg/mL (215.08 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years