sglt1

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).

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.

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

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.

Sotagliflozin (LX-4211, LP-802034) is an oral dual inhibitor of sodium-glucose cotransporter 1/2 (SGLT1/SGLT2) (SGLT2, IC₅₀ ≈ 1.8 nM; SGLT1, IC₅₀ ≈ 36 nM) used as an antidiabetic agent. Sotagliflozin is used in research on cardiovascular disease and diabetes.

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.

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

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-1 is a dual inhibitor of 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) .

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).

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.

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.

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.

Janagliflozin is an orally active and highly selective inhibitor of sodium-glucose co-transporter protein 2 (SGLT2) with an IC50 value of 0.0058 μM, and an IC50 of 4.802 μM for SGLT1. It inhibits SGLT2 in the proximal renal tubules, reducing glucose reabsorption and promoting urinary glucose excretion (UGE), thereby lowering blood glucose levels. Janagliflozin holds potential for research in treating type 2 diabetes.

Atigliflozin is an antihyperglycaemic drug candidate.

JNJ-39933673 is a bio-active chemical.

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.

TA-1887 is a new type of selective inhibitor of sglt2 for the treatment of type 2 diabetes. It has a significant hypoglycemic effect in KK (HF-KK) mice fed a high-fat diet. TA-1887 has good pharmacokinetic characteristics and significantly increases UGE

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.

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