sglt1

SGLT1 2-IN-1 is a dual inhibitor of SGLT1 and SGLT2.

SGLT1/2-IN-2 is a chemical compound with robust dual inhibitory properties, exhibiting potent activities against SGLT1 (IC50 = 96 nM) and SGLT2 (IC50 = 1.3 nM).

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).

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

Ipragliflozin (ASP1941) is under investigation in Type 2 Diabetes and Diabetes Mellitus, Type 2.

Sotagliflozin (LP-802034) is an orally bioavailable inhibitor of the sodium-glucose co-transporter subtype 1 (SGLT1) and 2 (SGLT2), with potential antihyperglycemic activity.

LX-2761 intermediate is a synthetic intermediate of LX-2761, a chemically stable and potent SGLT1/2 inhibitor.

LX-4211 intermediate is a synthetic intermediate of LX-4211, a potent SGLT1/2 inhibitor used as an antidiabetic agent.

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

Licogliflozin (LIK066) is an inhibitor of sodium-glucose cotransporter (SGLT1 and SGLT2).

Mizagliflozin (GSK-1614235 free base) is a sodium-glucose transporter inhibitor( Ki of 27 nM for human SGLT1). Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

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.

Trilobatin (P-Phlorizin) has anti-oxidant effect, can increase superoxide dismutase (SOD) activity.Trilobatin has anti-inflammatory effect, it potentially inhibits the lipopolysaccharide (LPS)-induced inflammatory response by suppressing the NF-κB signaling pathway.Trilobatin shows a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase for management of postprandial hyperglycemia with less side effect.

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.

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.

Henagliflozin (SHR3824) is an effective, oral, and selective SGLT2 inhibitor that effectively inhibits human SGLT2 in vitro, but has very weak inhibitory effects on human SGLT1.

Bexagliflozin (EGT1442) is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 2 nM for human SGLT2 and 5.6 μM for human SGLT1.

SAR-7226 Hydrate, a SGLT1/2 inhibitor, is used potentially for the treatment of type 2 diabetes.

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.

Ipragliflozin is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.

KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2 Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete.

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.