insulin receptor 1

NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.

[pTyr1146][pTyr1150][pTyr1151]Insulin Receptor (1142-1153) acts as a substrate for insulin receptor tyrosine kinase, binding effectively to insulin with potential applications in scientific research and medicine.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

Semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. This compound mimics GLP-1 to lower blood glucose levels and stimulates the growth of pancreatic β-cells responsible for insulin production and release. Additionally, Semaglutide inhibits the production of glucagon, a hormone that enhances glycogenolysis [the release of liver-stored carbohydrates] and gluconeogenesis [the synthesis of new glucose]. By reducing appetite and slowing gastric emptying, it also helps decrease food intake and aids in reducing body fat.

Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.

LSN3318839 is a small-molecule compound and a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), featuring oral activity and selective enhancement of G protein-coupled signaling, which promotes glucose-dependent insulin secretion for blood glucose reduction.

Liraglutide sodium salt is a glucagon-like peptide-1 (GLP-1) receptor agonist that, by mimicking the functions of endogenous GLP-1, promotes glucose-dependent insulin secretion in the pancreas and regulates appetite in the central nervous system, thereby effectively controlling blood glucose and reducing body weight.

Tirzepatide sodium is the sodium salt form of a dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist peptide drug that enhances insulin secretion and improves glycemic control by simultaneously activating GIP and GLP-1 receptors. In research and clinical settings, Tirzepatide sodium has also demonstrated effects in reducing body weight and improving metabolic parameters, and is used in studies related to type 2 diabetes and metabolic disorders.

Indirubin Derivative E804 is a potent insulin-like growth factor type 1 receptor (IGF1R) inhibitor with potential antitumor activity.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

NT219 is a dual inhibitor of insulin receptor substrate 1/2 (IRS1/2) and STAT3, enhances the aggregation of misfolded prion protein NT219 affects the levels of certain molecular chaperones and inhibits STAT3 phosphorylation NT219 is useful for the study of cancer and neurodegenerative diseases.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

Efpeglenatide is a long-acting agonist of the glucagon-like peptide-1 (GLP-1) receptor. Efpeglenatide improves insulin sensitivity, lowers blood glucose levels, and delays weight gain in diabetic and obese mouse models. Efpeglenatide has been applied in Type 2 diabetes research, providing an efficient experimental tool and preclinical evaluation value for developing metabolic disease intervention strategies, investigating weight loss mechanisms, and exploring insulin signaling regulation pathways.

AZD1979 is a highly potent MCHR1 (Melanin-concentrating hormone receptor 1) antagonist with an IC50 of 12 nM, exhibiting improved central nervous system (CNS) exposure and enhanced insulin sensitivity in steady-state model assessments, making it suitable for the treatment of obesity.

LY2922470 reduces glucose levels along with significant enhancements in insulin and GLP-1, which is the potential for the treatment of type 2 diabetes mellitus (T2DM). LY2922470 is an effective, selective, and orally available agonist of the G protein-cou

TUG-424 significantly enhances glucose-stimulated insulin secretion at 100 nM. TUG-424 is a potent and selective free fatty acid receptor 1 agonist (EC50: 32 nM).

INSR agonist 1, an insulin receptor (INSR) agonist, effectively elevates INSR pY1355/1361 levels and exhibits synergistic effects with insulin.

ZP3022 is a dual agonist targeting the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor. It selectively enhances cAMP accumulation or ERK phosphorylation in HEK293 cells with GLP-1R or CCK2 receptor expression, compared to ERK phosphorylation in cells with the CCK1 receptor (EC50s: 0.02, 10.3, and >1,000 nM for human receptors, respectively). At 40 nM, ZP3022 promotes proliferation of rat neonatal β-cells in vitro. It also boosts glucose-induced insulin secretion (GSIS) in rat pancreatic islets at 10 and 100 nM concentrations and decreases body weight in rats at 40 nmol/kg doses twice daily. Administered at 100 nmol/kg daily, ZP3022 enhances β-cell and total pancreatic mass and improves glucose tolerance in db/db mice, while reducing food intake but not body weight in these mice.

GLP-1R modulator-1 (Compound 384) is a potent and orally active selective agonist of the glucagon-like peptide-1 receptor (GLP-1R). It activates G protein-coupled signaling, leading to increased intracellular cAMP levels, enhanced insulin secretion, delayed gastric emptying, and reduced appetite. GLP-1R modulator-1 holds potential for research in type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

GLP-1R agonist 34 (Compound 1) is an orally active small molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R). It enhances insulin secretion, suppresses glucagon release, and slows gastric emptying, thereby effectively reducing blood glucose levels. GLP-1R agonist 34 holds potential for research into metabolic disorders such as type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH).

ZLN005 (hydrochloride) is an activator of the peroxisome proliferator-activated receptor-gamma coactivator 1-alpha (PGC-1α). It enhances the expression of PGC-1α and downstream genes in skeletal muscle cells, leading to improved glucose utilization and fatty acid oxidation. In diabetic db/db mice, ZLN005 (hydrochloride) elevates the transcription of PGC-1α and downstream genes in skeletal muscle, boosts fat oxidation, and enhances glucose tolerance, pyruvate tolerance, and insulin sensitivity.

BMS-577098 is an orally active ATP-competitive inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) with an IC50 value of 0.016 μM, exhibiting antitumor properties.