h-sglt2

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) 是一种特异性和口服活性的 hSGLT2 抑制剂，IC50 为 0.877 nM。 Ertugliflozin L-pyroglutamic acid 可用于治疗 2 型糖尿病的研究。

Dapagliflozin (BMS-512148) 是一种葡萄糖协同转运蛋白2 (SGLT2) 抑制剂，可与靶点竞争性结合。Dapagliflozin 可用于 2 型糖尿病的治疗，可以减少肾脏的葡萄糖重吸收，增加尿液中葡萄糖的排泄，从而降低血浆葡萄糖水平。

Canagliflozin (JNJ 28431754AAA) 是一种选择性 SGLT2 抑制剂，抑制表达 mSGLT2、rSGLT2 和 hSGLT2 的 CHO 细胞 (IC50=2 3.7 4.4 nM)。Canagliflozin 可以用于治疗 Ⅱ 型糖尿病 (T2DM)。

SGL5213 is an oral active and low-absorbable inhibitor of sodium-dependent glucose cotransporter 1 (SGLT1)(hSGLT1 and hSGLT2 with IC50 values of 29 nM and 20 nM , respectively),and has potential to treat type 2 diabetes.

Mizagliflozin 是口服有效的、选择性的 SGLT1抑制剂，对人 SGLT1 的 Ki 值为 27 nM。Mizagliflozin 对 SGLT1 的选择性是 SGLT2的303 倍。Mizagliflozin 是抗糖尿病药物，可以改善餐后血糖波动并有可能有改善慢性便秘的潜力。

SGLT inhibitor-1 is a potentsodium glucose co-transporter proteins (SGLTs) dual inhibitor(hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively).

LX2761 is a chemically stable and effective inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 (IC50s: 2.2 nM and 2.7nM for hSGLT1 and hSGLT2). However, it shows specific SGLT1 inhibition in the gastrointestinal (GI) tract.

Phlorizin (Phloridzin) 是非选择性的SGLT 抑制剂，也是Na+ K+-ATPase 抑制剂，对于hSGLT1和hSGLT2的Ki 值分别为 300 和 39 nM。

Ertugliflozin (PF-04971729) 是选择性的、口服有效的钠离子依赖的葡萄糖协同转运蛋白2 (SGLT2) 抑制剂，对h-SGLT2 的IC50值为 0.877 nM。Ertugliflozin 在2型糖尿病中有研究价值。

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK Ay type 2 diabetic mice, effects that were sustained even after 12 h.