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LX2761 在体外是一种化学稳定性和有效性的钠依赖性葡萄糖协同转运蛋白1 (SGLT1) 和 SGLT2 抑制剂,对hSGLT1 和 hSGLT2 的 IC50 值分别为 2.2 nM 和 2.7 nM,但在胃肠道 (GI) 表现出特定的 SGLT1 抑制作用。
LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract[1]. IC50: 2.2 nM (hSGLT1), 2.7nM (hSGLT2)[1]
[1]. Goodwin NC, et al. Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restrictedto the Intestinal Lumen, for the Treatment of Diabetes. J Med Chem. 2017 Jan 26;60(2):710-721.
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