sglt1

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

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1 4 5 6. Empagliflozin is used for the treatment of type 2 diabetes.

Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

SGLT1 2-IN-8 (compound 8) is a potent and orally active dual inhibitor of SGLT1 2, exhibiting IC50 values of 4 nM and 1 nM, respectively. It shows antihyperglycemic properties, making it suitable for related research.

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).

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

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

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

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.

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.

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.

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

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.

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.

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.

Bexagliflozin (also known as EGT1442) is a potent and selective SGLT2 inhibitor that effectively reduces blood glucose and HbA(1c) levels in db db mice while increasing the survival time of stroke-prone rats. The IC(50) values of EGT1442 for human SGLT1 and SGLT2 are 5.6 μM and 2 nM, respectively. In studies involving normal rats and dogs, EGT1442 induces saturated urinary glucose excretion with ED(50) values of 0.38 mg kg and 0.09 mg kg, respectively. Additionally, EGT1442 exhibits favorable properties in both in vivo and in vitro studies, indicating its potential positive impact on the management of type 2 diabetes.

Luseogliflozin, a potent and competitive inhibitor of sodium-dependent glucose cotransporter 2 (SGLT2), competitively inhibits human SGLT2-mediated glucose uptake with a Ki value of 1.10 nM.

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

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.

Atigliflozin is an antihyperglycaemic drug candidate.

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.