glut4

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.

β-Aminopropionitrile (3-Aminopropionitrile) is a selective inhibitor of lysyl oxidase.

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

GLUT4-IN-2 is a specific GLUT4 inhibitor that inhibits GLUT1 and GLUT4.GLUT4-IN-2 has antitumor activity, induces apoptosis and cell cycle arrest, and can be used for cancer research.

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.

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

1. Apigenin 7-glucoside (Cosmosiin) is a anti-HIV agent. 2. Cosmosiin may be beneficial for diabetic complications through their enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and GLUT4 translocation.

M617 acetate is a selective agonist of galanin receptor 1 (GAL1). M617 acetate acts through central GAL1, promotes GLUT4 expression, and enhances GLUT4 content in the cardiac muscle of type 2 diabetic rats. The Ki values are 0.23 and 5.71 nM for GAL1 and GAL2, respectively.

DCW-234, recognized as an ERbeta selective agonist, displays enhanced binding affinity for ERbeta over ERalpha, effectively promoting a strong, selective ERbeta SRC1 interaction. Studies have demonstrated that DCW-234 can induce GLUT4 expression in CHO-K1 cells.

Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.

Karanjin is a flavonoid obtained from the seeds of the karanja tree.Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.

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.

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).

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.

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 a hydroxylated C-16 or C-18 lipid. 9-PAHSA is a FAHFA in which palmitic acid is esterified to 9-hydroxy stearic acid. PAHSAs are the most abundant forms of FAHFA in serum as well as white and brown adipose tissues of glucose tolerant AG4OX mice, which overexpress Glut4 specifically in adipose tissue. 9-PAHSA is the predominant isomer of PAHSA in wild type and AG4OX mice. It is found in humans and is reduced in the serum and adipose tissues of insulin-resistant humans. 9-PAHSA improves glucose tolerance, stimulates insulin secretion, and has anti-inflammatory effects in mice.

1.(-)-Licarin B (Licarine B) has anti-mycobacterial activity.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg ml. Gliclazide (5 mg kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

M617 TFA, a selective galanin receptor 1 (GAL1) agonist, exhibits dissociation constants (Kis) of 0.23 nM for GAL1 and 5.71 nM for GAL2. Through activation of GAL1, M617 TFA enhances GLUT4 expression and content in the cardiac muscle of type 2 diabetic rats [1] [2].

10-OAHSA is a newly discovered endogenous lipid categorized within the group of branched fatty acid esters of hydroxy fatty acids (FAHFAs). This specific FAHFA comprises oleic acid esterified to 10-hydroxy stearic acid. It stands out among its FAHFA counterparts for its potential bioactive properties, similar to other members of its family such as PAHSAs, which are notably prevalent in the adipose tissue of AG4OX mice exhibiting glucose tolerance due to overexpression of the Glut4 glucose transporter specifically in adipose tissue. Like other FAHFAs, 10-OAHSA may play significant roles in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, which suggests its importance in managing metabolic syndrome and inflammation.

10-SAHSA, an endogenous lipid recently discovered, is part of the FAHFAs, a group of branched fatty acid esters of hydroxy fatty acids. It specifically consists of stearic acid esterified to 10-hydroxy stearic acid. Notably, PAHSAs, closely related to 10-SAHSA, are significantly present in the adipose tissue of AG4OX mice that are glucose tolerant due to the overexpression of the Glut4 glucose transporter in their adipose tissue. Similar to other FAHFAs, which are known to improve glucose tolerance, promote insulin secretion, and possess anti-inflammatory properties, 10-SAHSA is considered a potential bioactive lipid with implications for metabolic syndrome and inflammation management.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids influenced by dietary changes, playing a crucial role in insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid (for example, palmitoleic, palmitic, oleic, or stearic acid) linked to a hydroxy fatty acid with the same carbon chain length. 13-PAHSA, a derivative where palmitic acid is esterified to 13-hydroxy stearic acid, is notably prevalent in the adipose tissue of glucose-tolerant AG4OX mice, which exhibit enhanced glucose transport via the overexpression of the Glut4 glucose transporter. This observation, along with the metabolic benefits seen from other FAHFAs—including improved glucose tolerance, stimulated insulin secretion, and anti-inflammatory properties—suggests that 13-PAHSA may function as a bioactive lipid beneficial in managing metabolic syndrome and inflammation.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets, and they play a role in insulin sensitivity. These compounds consist of a fatty acid—either a C-16 or C-18, such as palmitoleic, palmitic, oleic, or stearic acid—esterified to a hydroxylated C-16 or C-18 lipid. One notable FAHFA, 9-PAHSA, features an ester linkage between palmitic acid and 9-hydroxy stearic acid. PAHSAs, with 9-PAHSA being the most prevalent isomer, are significantly found in the serum and both white and brown adipose tissues of glucose-tolerant AG4OX mice, which express the Glut4 gene in adipose tissue, enhancing insulin sensitivity. Additionally, 9-PAHSA is abundant in wild type and AG4OX mice and present in humans, though at reduced levels in those with insulin resistance. 9-PAHSA is associated with improved glucose tolerance, enhanced insulin secretion, and anti-inflammatory effects in mice. The compound 19-PAHSA^13C4 represents an isotopically enriched form of this polyunsaturated fatty acid.

13-SAHSA, a branched fatty acid ester of hydroxy fatty acids (FAHFAs), has been found to be involved in metabolic regulation, particularly in relation to fasting, high-fat feeding, and insulin sensitivity. This compound is a synthesis of stearic acid and 13-hydroxy stearic acid. Notably, 13-SAHSA levels are found to be moderately increased in the serum of AG4OX mice, which are characterized by their glucose tolerance and expression of the Glut4 glucose transporter specifically in their adipose tissue. Similar to other FAHFAs, 13-SAHSA is believed to play a significant role in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, indicating its potential importance in addressing conditions related to metabolic syndrome and inflammation.