NPS-2143 is a selective antagonist of calcium-sensing receptor (CaSR) with an IC50 of 43 nM.
ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK).
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A[1].
Prosaikogenin F is a monoglycoside with anticancer and hemolytic properties[1][2].
Neoisoastilbin possesses antioxidant, anti-hyperuricemic and anti-Inflammatory activities[1].
Validamine competitively inhibits β-glucosidase in a pH-dependent and dose-dependent manner, with an IC50 value of 2.92mM, and the maximum inhibitory ability is at the optimum pH value of this enzyme[1].
Phosphocreatine, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives, is a substrate for the determination of creatine kinase and used to regenerate ATP during skeletal muscle contraction[1]..
DPP-4/GPR119 modulator 1 (Compound 22) is an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist. DPP-4/GPR119 modulator 1 shows blood glucose-lowering effect and moderate inhibition on hERG channel with an IC50 of 4.9 µM. DPP-4/GPR119 modulator 1 can be used for diabetes research[1][1].
Desmethylicaritin is a phytoestrogenic molecule, has inducible effect on directional differentiation of embryonic stem cells into cardiomyocytes. Desmethylicaritin also suppresses adipogenesis via Wnt/β-catenin signaling pathway[1][2].
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2].
1,2,3,6-Tetragalloylglucose is a potent UDP glucuronosyltransferase 1 family, polypeptide A1 (UGT1A1) inhibitor, with a Ki of 1.68 μM[1].
FKKSFKL-NH2 is a protein kinase C-selective peptide. FKKSFKL-NH2 can be used for the research of various biochemical[1].
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO- scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease[1]. Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways[2]. Epiberberine has the potential effect in the research of diabetic disease[3].
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases[1].
Glucagon exhibits marked effects on protein and amino acid metabolism. Glucagon inhibits the incorporation of amino acids into protein of liver, muscle, and pancreas, to increase excretion of nitrogen, to promote hepatic urea synthesis, and to increase the concentration of hepatic transaminases and urea cycle enzymes. Glucagon can promote the hepatic uptake of amino acids, to enhance their incorporation into liver glycogen, and to depress the concentration of amino acids in blood[1].
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases[1].
Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity[1][2][3].
1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production.
N-(5-Amino-1-ribosyl-4-imidazolecarbonyl)-L-aspartic acid is a nucleoside metabolite[1].
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases[1].
Cisd2 agonist 1 (Compound 4q) is a Cisd2 agonist (EC50: 34 nM). Cisd2 agonist 1 enhances the Cisd2 expression and improves the pathological changes in the fatty livers. Cisd2 agonist 1 has good metabolic stability. Cisd2 agonist 1 can be used for research of NAFLD[1].
Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor.
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU)[1].
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1].
Salvifaricin is an orally active diterpenoid compound that can be isolated from Salvia leucantha Cav. and Salvia hispanica L.. Salvifaricin significantly reduces fasting blood glucose and serum triglyceride (TG) levels, and has anti-diabetic effect[1][2].
BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.
Utreglutide is a potent glucagon-like peptide 1 (GLP-1) receptor agonit[1].
Mogroside III-A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities[1].
Buprofezin-d6 is the deuterium labeled Buprofezin. Buprofezin is a broad-spectrum insecticide and chitin synthesis inhibitor that targets developmental stage coleopteran pests.Buprofezin promotes the conversion of energy metabolism from the aerobic tricarboxylic acid (TCA) cycle and oxidative phosphorylation to anaerobic glycolysis. Buprofezin also promotes the production of reactive oxygen species (ROS) by inhibiting cytochrome c oxidase[1][2].
Glucocerebrosidase-IN-1 (compound 11a) is a potent and selective GCase (glucocerebrosidase) inhibitor, with an IC50 of 29.3 μM and a Ki of 18.5 μM. Glucocerebrosidase-IN-1 can be used for the research of Gaucher disease (GD) and Parkinson’s disease (PD)[1].