Iinerixibat (GSK2330672) is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) which lowers glucose in an animal model of type 2 diabetes and shows excellent developability properties for evaluating the potential therapeutic utility of a nonabsorbable ASBT inhibitor for treatment of patients with type 2 diabetes.
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.
yGsy2p-IN-H23 is a potent and first-in-class inhibitor for yeast glycogen synthase 2 (yGsy2p) with an IC50 of 875 µM for human glycogen synthase 1 (hGYS1). yGsy2p-IN-H23 bounds within the uridine diphosphate glucose binding pocket of yGsy2p. yGsy2p-IN-H23 is used for glycogen storage diseases (GSDs)[1].
Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities.
Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC50 values of 2.1 and 6.1 nM, respectively.
rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1 receptor antagonist. rel-O-2050 also decreases food intake in mice[1].
Demethylcantharidate disodium, an endogenous metabolite, induces apoptosis in hepatocellular carcinoma cells via ER stress. Demethylcantharidate disodium shows excellent anticancer activity against multiple types of cancer[1].
Glutarylcarnitine is the diagnostic metabolite for malonic aciduria and glutaric aciduria type I monitored in most tandem mass spectrometry newborn screening programmes.
4-Methoxybenzimidamide is a reagent used for the determination of reducing carbohydrates and glycoproteins.
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3].
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect[1].
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice.Glycyrin also shows antibacterial activity[1][2][3].
2-Phenylglycine (DL-α-Phenylglycine) is a metabolite in breast milk during the W2 to W4 lactation period[1].
L-Tryptophan-1-13C (Tryptophan-1-13C) is the 13C-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect[1].
Picornain 3C is a protease found in picornaviruses, which cleaves peptide bonds of non-terminal sequences. Picornain 3C is an intermediate between the serine peptidase chymotrypsin and the cysteine peptidase papain. Picornain 3C shows endopeptidase activity by selectively cleaving Gln-Gly bonds in the polyprotein of poliovirus and with substitution of Glu for Gln, and Ser or Thr for Gly in other picornaviruses[1].
10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM[1].
Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly;HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG.
Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides[1].
Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots[1]. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades[2].
MID-1 is an inhibitor of MG53-IRS-1 (Mitsugumin 53-Insulin Receptor Substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake[1].
a-FABP-IN-1 (Compound 5g) is a potent and selective human adipocyte fatty acid-binding protein (a-FABP) inhibitor with a Ki below 1.0 nM. a-FABP-IN-1 inhibits the pro-inflammatory cytokine production[1].
MK-0941 free base is an orally active glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes[1][2].
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively [1].
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.
LG 82-4-01 is a thromboxane (TX) synthetase specific inhibitor, with an IC50 of 1.3 μM[1].
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect[1][2][3][4].
Kaempferol 3-sophoroside-7-glucoside is a bioactive component in roasted Lycium chinense leaves with anti-obesity activity[1].
Repaglinide(AG-EE 623ZW) is a carbamoylmethyl benzoic acid (CMBA) derivative, which recently has become available for the treatment of type II diabetes. IC50 value:Target: Repaglinide is very rapidly absorbed (tmax less than 1 hour) with a t1/2 of less than one hour. Furthermore, repaglinide is inactivated in the liver and more than 90 % excreted via the bile. Repaglinide (1 mg/kg p.o.) was effective (P < 0.001) as an insulin-releasing agent in a rat model (low-dose streptozotocin) of type 2 diabetes.