glucose transporter

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

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.

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.

STF-31 is an inhibitor of glucose transporter 1 (GLUT1) with IC50 of 1 μM.

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

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Remogliflozin is an effective sodium-glucose transporter 2 inhibitor (Kis = 12.4 and 26 nM for human and rat SGLT2, respectively).

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

Dapagliflozin impurity is the enantiomer of Dapagliflozin, Dapagliflozin is a sodium glucose transporter 2 inhibitor.

GLUT4 activator 1 is a potent glucose transporter type 4 (GLUT4) translocation activator (EC50: 0.14 μM).

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).

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.

GLUT-1-IN-4 (Compound 13) is an inhibitor of the GLUT-1 glucose transporter that depends on the p53 protein. It suppresses the proliferation of various cancer cells at submicromolar IC50 levels. Additionally, GLUT-1-IN-4 can halt the cell cycle, induce oxidative stress, and promote apoptosis (cell death).

Olorigliflozin is a sodium glucose co-transporter (SGLT) inhibitor with antihyperglycemic properties.

DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1 S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].

YM-543, a sodium-glucose transporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.

MitoPQ (MitoParaquat) is a mitochondria-targeted small molecule compound that selectively enhances mitochondrial superoxide and hydrogen peroxide levels and inhibits insulin-stimulated glucose uptake and translocation of glucose transport protein 4 (GLUT4) to the plasma membrane in adipocytes and myotubes.MitoPQ can be used to MitoPQ can be used to study mitochondrial oxidative stress and regulated GLUT4 transporter.

10-PAHSA is a newly identified endogenous lipid that belongs to a collection of branched fatty acid esters of hydroxy fatty acids (FAHFAs). It is a FAHFA in which palmitic acid is esterified to 10-hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. As other FAHFAs improve glucose tolerance, stimulate insulin secretion, and have anti-inflammatory effects, 10-PAHSA may be a bioactive lipid with roles in metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are newly identified endogenous lipids regulated by fasting and high-fat feeding and associated with insulin sensitivity. Structurally, these esters are comprised of a C-16 or C-18 fatty acid (e.g., palmitoleic, palmitic, oleic, or stearic acid) linked to either a C-16 or C-18 hydroxy substituent. 12-PAHSA is a FAHFA in which palmitic acid is esterified at the 12th carbon of hydroxy stearic acid. Among the FAHFA family members, PAHSAs are the most abundant in the adipose tissue of glucose tolerant AG4OX mice, which overexpress the Glut4 glucose transporter specifically in adipose tissue. 12-PAHSA is present at 2- to 3-fold higher levels in adipose tissue of AG4OX mice compared to wild type mice. Levels of 12-PAHSA are also higher in fasted wild-type mice compared to fed mice and are reduced upon high-fat diet-induced obesity in insulin-resistant mice.

ADP-Glucose (ADPG) is an immediate precursor used in the biosynthesis, by glucose addition, of storage polysaccharides in plants, green algae, and cyanobacteria, as well as structural polysaccharides in certain bacteria.[1],[2] It is used by amylose synthases or starch synthases in plastids in the production of amylose, amylopectins, starch, and other polysaccharides. ADPG is normally generated within plastids, although it can be biosynthesized in the cytoplasm of certain grasses and imported into plastids by a membrane-bound transporter.[3]

Luseogliflozin (TS 071) hydrate, a second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor, exhibits selective potency and oral activity, with an IC50 of 2.26 nM. This compound is utilized in research for the treatment of type 2 diabetes mellitus (T2DM).

Enavogliflozin (DWP-16001) is an orally available small molecule and sodium glucose transporter 2 inhibitor.