glucose-dependent

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

Gastric Inhibitory Peptide (1-42) (porcine) TFA is a glucose-dependent insulinotropic polypeptide released by intestinal K-cells. It stimulates insulin secretion while inhibiting gastric acid secretion and gastrointestinal motility, thereby regulating digestive function.

Gastric inhibitory peptide 1 (GIP-1) (3-42), a fragment of the incretin hormone GIP and antagonist to the GIP receptor, is generated through the action of serum dipeptidyl peptidase 4 (DDP-4). When administered at 25 nmol/kg to an ob/ob mouse diabetes model, GIP-1 (3-42) elevates plasma glucose levels and lowers plasma insulin levels, demonstrating its effect on reducing insulin secretion from BRIN-BD11 pancreatic cells at a concentration of 100 nM.

Gastric inhibitory peptide (GIP) (22-51), a pro-atherogenic peptide comprised of 30 amino acids from the residues 22-51 of its precursor protein proGIP, is present in human plasma. It activates the degradation of IκB-α and the nuclear translocation of NF-κB in both macrophage-differentiated THP-1 cells and human aortic endothelial cells at a concentration of 1 µM. Additionally, in ApoE-/- mice, GIP (22-51) escalates the area of atherosclerotic lesions and plaque development in vivo.

GIP (22-51) human (Glucose-dependent Insulinotropic Peptide (22-51) human) is a potent pro-atherosclerotic peptide hormone composed of 30 amino acids. It activates the NF-κB signaling pathway, enhances the expression of MMP-8, and induces the expression of pro-inflammatory and pro-atherogenic proteins. Additionally, it increases intracellular free Ca2+ levels in THP-1 induced macrophages. GIP (22-51) human is useful for atherosclerosis research.

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.

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

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

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.

Tirzepatide (LY3298176) is a long-acting glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor dual agonist. In HEK293 cells, it can effectively stimulate cAMP accumulation, with an EC50 of 0.0224 nM for the GIP receptor (GIPR) and an EC50 of 0.934 nM for the GLP-1 receptor (GLP-1R).

Tirzepatide (LY3298176) Acetate (2023788-19-2 free base) is a new molecule that can control blood glucose levels by combining dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors.[3]

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

NCT-502 (N-(4,6-dimethylpyridin-2-yl)-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine-1-carbothioamide) is a human phosphoglycerate dehydrogenase inhibitor, cytotoxic to PHGDH-dependent cancer cells. It decreases glucose-derived serine production and it has an IC50 of 3.7 μM against PHGDH.

α-NETA is a potent choline acetyltransferase (ChA) inhibitor and an ALDH1A1 and chemokine-like receptor 1 (CMKLR1) antagonist.Anti-cancer activity,Cholinesterase and acetylcholinesterase (AChE) inhibition,Dose-dependent reduction of body weight and fasting blood glucose levels in STZ-induced diabetic mice,Significantly reduced expression of renal injury markers,May be CEP-9722 can be used for the study of diabetic nephropathy.

Suksdorfin has hypoglycemic effects, promotes adipocyte differentiation and enhances lipocalin production, activates peroxisome proliferator-activated receptor gamma (PPARγ), promotes insulin-dependent glucose uptake by adipocytes, and can be used to study obesity.

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a selective and orally active hSGLT2 inhibitor with an IC50 of 0.877 nM, suitable for studies on the treatment of type 2 diabetes mellitus.

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).

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) .

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.

(2S,3R,4S)-4-Hydroxyisoleucine (Hydroxyisoleucine) from fenugreek (Trigonella foenum-graecum) seeds is a potential insulinotropic (anti-diabetic) and anti-obesity amino acid that stimulates glucose-dependent insulin secretion from pancreatic cells, activates insulin receptor substrate-associated phosphoinositide 3 (PI3) kinase activity, and reduces plasma levels of triglycerides, free fatty acids, and cholesterol.

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.