pancreatic β cell

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Imeglimin (EMD 387008) is an orally available antidiabetic compound that enhances mitochondrial function, enhances insulin secretion, promotes β-cell proliferation and improves pancreatic β-cell survival in mice.

RH01687 is a potent β-cell protector , exhibits β-cell-protective activities against endoplasmic reticulum (ER) stress.

Kazinol U may have therapeutic value in delaying pancreatic β-cell destruction in type 1 diabetes by blocking the NF-κB pathway in pancreatic β-cells reduces cell damage. Kazinol U shows estrogenic activity with ligand-activity of estrogen receptor, transcriptional activity of estrogen -responsive element-reporter genes, it may have beneficial effects in the treatment of menopausal symptoms.

Linogliride fumarate is the fumarate salt of Linogliride. Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in glucose turnover.

GIP, rat TFA (glucose-dependent insulinotropic polypeptide), a 42-amino acid peptide secreted by K cells in the duodenum and jejunum, promotes insulin release from pancreatic beta cells, supports beta cell proliferation, and enhances their survival. This rat-origin bioactive peptide, along with GLP (gastric-like peptide), belongs to the intestinal insulinotropic hormone family and is implicated in lipid homeostasis and potentially in the pathogenesis of obesity. Recent research suggests GIP's multifaceted role in these metabolic processes.

Vin-C01 can be used for the research of type 2 diabetes mellitus that is a potent protective agent of pancreatic β-cells (EC 50 = 0.22 μM). Vin-C01 effectively protects β-cells from apoptosis induced by STZ and promotes β-cell survival [1].

BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT

Amylin (1-37) (human) (hIAPP (1-37)), a peptide hormone located in pancreatic beta-cell secretory granules, is characterized by an amidated C-terminus and a disulfide bond between cysteine residues 2 and 7 [1].

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5

Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor noted for its anti-diabetic activity. It enhances pancreatic beta-cell proliferation, boosts insulin secretion, and lowers blood glucose levels.

WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-

BDC2.5 Mimotope 1040-63 is a biologically active peptide used in the investigation of type 1 diabetes (T1D), an autoimmune disease where T cells induce destruction of pancreatic islet β cells. This mimotope, originating from the TCR transgenic model (BDC2.5), facilitates the examination of antigen presentation mechanisms to islet autoantigen-specific T cells, contributing to the understanding of T cell-mediated beta-cell damage due to autoreactive T cell responses.

Vin-F03 can be used in the research of type 2 diabetes mellitus that is an effective protective agent of pancreatic β-cells (EC50 = 0.27 μM). Vin-F03 potently promotes the survival of β-cell and protects β-cells from apoptosis induced by STZ[1].

GKA50 quarterhydrate is a potent glucokinase activator with an EC50 value of 33 nM. This glucose-like activator of β-cell metabolism in rodent and human pancreatic islets is a Ca2+-dependent regulator of insulin secretion. It stimulates insulin secretion in mouse islets and significantly reduces blood glucose in high-fat-fed female rats.

Dorzagliatin (HMS5552) is a dual-acting glucokinase (GK) activator. It also improves glycaemic control and pancreatic β-cell function in type 2 diabetes.

Amylin, amide, human is a 37-amino acid peptide hormone co-secreted with insulin to regulate postprandial glucose levels, reducing glucagon secretion and delays gastric emptying. DAP Amide's tendency to aggregate into amyloid fibrils is associated with pancreatic β-cell damage in type 2 diabetes.

Amylin (8-37), human, derived from human Amylin, possesses direct vasodilator effects in isolated mesenteric resistance arteries of rats. Human Amylin is a small pancreatic β-cell hormone that forms aggregates in the absence of insulin and is a key pathological feature of type II diabetes mellitus.

Nephrin is a cell surface signaling receptor protein that regulates podocyte function and plays a role in β-cell survival signaling; it is a protein necessary for the proper functioning of the renal filtration barrier. Nephrin belongs to a family of highl

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).