hsglt1

Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2 3.7 4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).

Phlorizin (Phloridzin) is a non-selective SGLT inhibitor found in apple, for hSGLT1( Ki=300 nM) and hSGLT2( Ki=39 nM) .

Mizagliflozin is an orally active, selective SGLT1 inhibitor with a Ki value of 27 nM for human SGLT1. Mizagliflozin is 303 times more selective for SGLT1 than for SGLT2. Mizagliflozin is an anti-diabetic drug that can improve postprandial blood sugar fluctuations and may have the potential to improve chronic constipation.

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.

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.

Remogliflozin etabonate (GSK189075A) is a prodrug of regaliflozin and an inhibitor SGLT2 with Ki values of 1.95, 2.14, 8.57, and 43.1μM for hSGLT2, rSGLT2, rSGLT1, and hSGLT1, respectively.

TP0438836 is a potent, low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor for the treatment of type 2 diabetes. TP0438836 showed IC50 values 28nM and 7 nM for hSGLT1 and hSGLT2 resepctively.