insulin secretion

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

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.

GIP (1-39) acetate is a gastric inhibitory peptide (GIP) purified from porcine intestine and stimulates insulin secretion.

RH01386 is a small molecule that prevents ER stress-induced β cell dysfunction and death, inhibits proapoptotic gene expression, and restores ER stress-impaired glucose-stimulated insulin secretion responses, showing potential for type 2 diabetes treatment.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

LY2881835 is a potent and selective GPR40 agonist.

Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

Vincamine (Perval) is a major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cerebrovascular disorders.

Mitiglinide calcium hydrate (S-21403 calcium hydrate) is a drug for the treatment of type 2 diabetes. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs and is currently co-marketed in Japan by Kissei and Takeda.

Nateglinide (Senaglinide) is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury.

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.

trans-Cinnamic acid (Myricitrine) exerts anti-diabetic activity by improving glucose tolerance in vivo and by stimulating insulin secretion in vitro.

(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.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).

Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) is a triacylglycerol found in dietary fats. In hamsters fed a diet enriched with it, Tripalmitin increases body weight, elevates plasma LDL levels, and reduces hepatic LDL receptor mRNA levels. It inhibits glucose-stimulated insulin secretion and decreases the viability of INS1 cells dose-dependently. Tripalmitin is used in cosmetic products for skin conditioning and as a thickening agent, and it forms lipid matrices of nanoparticles for drug delivery.

AM-4668, a GPR40 (FFA1) agonist with oral availability, was optimized to reduce central nervous system (CNS) permeability, with a mouse brain plasma ratio of only 0.02, and significantly reduced blood glucose levels in human GPR40 knock-in mice.

RO-28-1675 is a direct and selective glucokinase activator that indirectly affects the activity of the GK GKRP (glucokinase regulatory protein) complex, with efficacy decreasing with increasing glucose concentration, and can be used in studies related to insulin secretion and type 2 diabetes.

Galantide acetate, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide acetate recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide acetate dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide acetate appears to bind to a single population of SP receptors (KD~40 nM).

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

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

GSK137647A (GSK 137647) is a selective agonist of FFA4.

Chikusetsusaponin IVa (Calenduloside F) is a novel AMPK activator, can induce insulin secretion from βTC3 cells via GPR4 mediated calcium and PKC pathways, may be developed into a new potential for therapeutic agent used in T2DM patients.

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.