Remogliflozin etabonate (GSK189075) is an orally active, selective, and low-affinity sodium glucose cotransporter (SGLT2) inhibitor, with Ki values of 1.95 μM, 2.14 μM, 43.1 μM, and 8.57 μM for hSGLT2, rSGLT2, hSGLT1, and rSGLT1, respectively. It is a prodrug based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, within the body. This compound demonstrates antidiabetic efficacy in rodent models[1].
体内研究
Remogliflozin etabonate (GSK189075; 10 or 30 mg/kg; orally; administered twice daily for 6 weeks) significantly lowers both fasting plasma glucose (FPG) and glycosylated hemoglobin (GHb) levels in a dose-dependent manner[1].
Oral administration of Remogliflozin etabonate (at doses of 3, 10, and 30 mg/kg) leads to a dose-dependent increase in urinary glucose excretion. Additionally, Remogliflozin etabonate dose-dependently inhibits the rise in plasma glucose levels following glucose loading and decreases plasma insulin levels in normal rats[1].
Remogliflozin etabonate (at doses ranging from 1 to 10 mg/kg; orally) reduces blood glucose levels and diminishes the area under the curve (AUC0–6 h) for blood glucose in a dose-dependent manner[1].
Remogliflozin etabonate (administered via a high-fat diet containing 0.01%, 0.03%, or 0.1% remogliflozin etabonate for 8 weeks) reduces plasma glucose, plasma insulin, and glycosylated hemoglobin (GHb) levels in male GK rats (6 weeks of age) in a dose-dependent manner. Additionally, it inhibits the development of hypertriglyceridemia[1].
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