Insulin Receptor Activator

Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Semaglutide acetate is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide acetate promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide acetate also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide acetate has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide acetate can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Morin is an orally active plant-derived flavonoid. Morin inhibits ROS generation. Morin induces Apoptosis. Morin inhibits PTP1B (IC₅₀ of 15 μM) and activates the insulin receptor. Morin has a detoxifying effect. Morin can be used in diabetes, leukemia, colon cancer, cervical cancer, Parkinson's disease and hypertension research.

Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.

Ligandrol is an orally active, selective androgen receptor (AR) agonist. Ligandrol enhances protein synthesis, inhibits muscle breakdown and oxidative stress, improves muscle cell viability and bone tissue microstructure, and reduces Cisplatin (HY-17394)-induced muscle toxicity and apoptosis. Ligandrol promotes muscle growth, protects bone structure, and has anti-diabetic, anti-apoptotic and antioxidant effects. Ligandrol can antagonize Streptozotocin (HY-13753) damage to pancreatic islets and improve the symptoms of type 2 diabetes.

Kaempferitrin is a natural flavonoid, possesses antinociceptive, anti-inflammatory, anti-diabetic, antitumoral and chemopreventive effects, and activates insulin signaling pathway.

Semaglutide-¹³C₆,¹⁵N TFA is the ¹³C- and ¹⁵N-labeled Semaglutide TFA (HY-114118A). Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Panaxatriol is an orally active dammarane-type tetracyclic triterpene sapogenin. Panaxatriol enhances the phosphorylation levels of Akt, insulin receptor and p70S6K in skeletal muscle. Panaxatriol reduces the mRNA expression level of Atrogin1 in skeletal muscle. Panaxatriol induces apoptosis, pre-G1 cell cycle arrest and increased intracellular ROS levels in prostate cancer cells, decreases mitochondrial membrane potential, inhibits cell migration and reduces colony formation. Panaxatriol can be used in research related to insulin resistance, myocardial ischemia/reperfusion injury and prostate cancer^[1][2][3].

BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.

Semaglutide (crude) is the crude form of Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances Autophagy, inhibits oxidative stress and Apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

Biguanide is an orally active antihyperglycemic agent. Biguanide inhibits mitochondrial ATP production, activates the LKB1-AMPK signaling pathway, and damages the energy homeostasis. Biguanide enhances insulin-receptor activation and downstream signaling. Biguanide exhibits potential in ameliorating the type 2 diabetes and the insulin-associated cancers.

CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model.

Demethylasterriquinone B1 (DAQ B1; L-783281) is an orally active insulin receptor (insulin receptor) agonist and AKT activator. By activating AKT, Demethylasterriquinone B1 upregulates the expression and activity of eNOS to increase NO production, while downregulating the expression of the NADPH oxidase subunit p22phox to reduce oxidative stress and improve vascular endothelial dysfunction in hypertensive rats. Demethylasterriquinone B1 combind with an AKT inhibitor targets the insulin signaling pathway to activate two antiviral pathways, RNA interference and JAK/STAT, in mosquitoes, thereby reducing Zika virus infection.

Semaglutide-d₈ tetraTFA is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.

GLUT4 activator 2 (C59) is an insulin sensitizer, which can be used for research of diabetic diseases. GLUT4 activator 2 improves glucose uptake and insulin sensitivity in rodents. GLUT4 activator 2 interacts with Unc119 and Unc119B resulting in increased insulin sensitivity and GLUT4 translocation.

Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside) is a flavonoid. Kaempferol 3-neohesperidoside mimics insulin action via the PI3K/PKC pathway, significantly promoting glucose uptake and increasing muscle glycogen content in rat soleus muscles. Kaempferol 3-neohesperidoside also exhibits anti-glycation activity. Kaempferol 3-neohesperidoside binds to albumin through hydrogen bonding and hydrophobic interactions, and inhibits the formation of advanced glycation end products. Kaempferol 3-neohesperidoside can be used in studies of diabetes and its related complications.

L-Ornithine 2-oxoglutarate (Ornithine alpha-ketoglutarate) is a nutritional compound that is a salt of amino acids with antioxidant and anti-inflammatory effects. L-Ornithine 2-oxoglutarate stimulates the production of insulin and growth hormone, and promotes intracellular amino acid transport and protein synthesis.

Sequoyitol (5-O-Methyl-myo-inositol) is an orally active hypoglycemic agent and antioxidant. Sequoyitol can be isolated from herbaceous plants. Sequoyitol downregulates the expression of NF-κB and TGF-β1, reduces ROS production and malondialdehyde levels, and enhances total antioxidant capacity. Sequoyitol activates the insulin signaling pathway, including the phosphorylation of IR, IRS1 and Akt. Sequoyitol increases serum insulin levels, inhibits hepatic glucose production, and promotes cellular glucose uptake. Sequoyitol antagonizes TNFα-induced inhibition of the insulin signaling pathway, and decreases blood urea nitrogen and serum creatinine levels. Sequoyitol elicits potential peaks in the chemosensors of adult and larval Atrophaneura alcinous, and acts as an oviposition stimulant for female Atrophaneura alcinous. Sequoyitol can be used in research related to type 2 diabetes, insulin resistance, hyperglycemia, impaired glucose tolerance and diabetic nephropathy.

TLK19781 is a non-peptide small molecule insulin receptor activator that increases the content of insulin-stimulated GLUT4 on the cell membrane and enhances the activity of insulin-stimulated glucose transport in cell and animal models of insulin resistance.