Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
FATP1-IN-1 is a fatty acid transport protein 1 (FATP1) inhibitor. FATP1-IN-1 is an inhibition of recombinant human or mouse acyl-CoA synthetase activity of FATP1, with the IC50 values of 0.046 μM or 0.60 μM, respectively[1].
Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over allproteases tested (IC50 > 67 μM).IC50 value: 1.6 nM [1]Target: DPP-4 inhibitorin vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).
Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis[1][2][3].
neo-Inositol, a stereoisomer of inositol, has been isolated from calf brain[1].
Mogroside IV, 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].
Pyruvate kinase is a glycolytic enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP[1].
Levoglucosan-d7 is the deuterium labeled Levoglucosan. Levoglucosan (1,6-Anhydro-β-D-glucopyranose) is an anhydrosugar produced through glucan pyrolysis and is widely found in nature[1][2].
(Des-Gly2)-Exenatide is a potential impurity of Exenatide (HY-13443).
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.IC50 value: 43 nM(for Ca2+ receptor) [1]Target: CaSRin vitro: NPS 2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS 2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH [1]. The first reported calcilytic compound was NPS 2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH [2].in vivo: When infused intravenously in normal rats, NPS 2143 caused a rapid and large increase in plasma levels of PTH. Ca2+ receptor antagonists are termed calcilytics and NPS 2143 is the first substance (either atomic or molecular) shown to possess such activity [1]. When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats [2].
Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC50 of 25 nM[1].
2-Bromoacetamide can inactivate alcohol dehydrogenase[1].
BMS-986172 is an orally active, highly selective MGAT2 inhibitor with an IC50 of 4.6 nM and 20 nM for hMGAT2 and mMGAT2, respectively. BMS-986172 has a T1/2>120 min in vitro assays. BMS-986172 reduces food intake and body weight. BMS-986172 has the potential for metabolic disorders such as obesity and NASH research[1].
Glomeratide A is a benzophenone C-glucoside with hepatoprotective effects. Glomeratide A has a protective effect against d-galactosamine-induced hepatotoxicity in rat liver epithelial stem-like cells.
Galanin-Like Peptide (human) is a 60 amino acid neuropeptide. Galanin-Like Peptide (human) plays an important role in the regulation of feeding, body weight and energy metabolism[1].
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R).
3-Pyridinemethanol (Nicotinyl alcohol), a pyridine derivative, is a cholesterol-lowering agent[1][2].
UDP-GalNAz disodium (UDP-N-azidoacetylgalactosamine disodium) is the analogue of UDP-GalNAc. UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor[1].
CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research[1].
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies[1].
13Z,16Z-Docosadienoic acid, a ω-6 polyunsaturated fatty acid, possesses anti-borreliae effect. 13Z,16Z-Docosadienoic acid, as a long-chain fatty acid (LCFA), is a free fatty acid receptor 4 (FFAR4 or GPR120, a LCFA receptor) agonist[1].
Casanthranol is a concentrated mixture of anthranol glycosides from cascara sagrada (dried bark of Rhamnus p.) and used as a laxative in constipation and various medical conditions, stimulant laxative Casanthranol encourages bowel movements by acting on the intestinal wall to increase muscle contractions[1].
AZ1729 is a novel direct, positive allosteric modulator of fatty acid receptor FFA2 (pEC50=6.9), selectively activates Gi signaling but lacks the capacity to activate FFA2 Gq/G11-mediated signaling pathways; produces stimulation of [35S]GTPγS binding with pEC50 7.23, inhibits β-adrenoreceptor agonist-promoted lipolysis in primary mouse adipocytes and promotes chemotaxis of isolated human neutrophils.
This enzyme is the product of the Lewis blood group gene. Normally acts on a glycoconjugate where R (see reaction) is a glycoprotein or glycolipid. Although it is a 4-fucosyltransferase, it has a persistent 3-fucosyltransferase activity towards the glucose residue in free lactose. This enzyme fucosylates on O-4 of an N-acetylglucosamine that carries a galactosyl group on O-3, unlike EC 2.4.1.152, 4-galactosyl-N-acetylglucosaminide 3-α-L-fucosyltransferase, which fucosylates on O-3 of an N-acetylglucosamine that carries a galactosyl group on O-4. Enzymes catalysing the 4-α-fucosylation of the GlcNAc in β-D-Gal-(1→3)-β-GlcNAc sequences (with some activity also as 3-α-fucosyltransferases) are present in plants, where the function in vivo is the modification of N-glycans. In addition, the fucTa gene of Helicobacter strain UA948 encodes a fucosyltransferase with both 3-α- and 4-α-fucosyltransferase activities. Reaction: GDP-β-L-fucose + β-D-galactosyl-(1→3)-N-acetyl-D-glucosaminyl-R = GDP + β-D-galactosyl-(1→3)-[α-L-fucosyl-(1→4)]-N-acetyl-β-D-glucosaminyl-R
Atorvastatin sodium is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin sodium inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively[1][2][3][4][5].
Insulin efsitora alfa (LY-3209590) is a selective agonist of insulin receptor (IR). Insulin efsitora alfa is a fusion protein composed of human IR agonists fused with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2) fragment, with a molecular weight of 64.1 kDa. Insulin efsitora alfa is well tolerated and has potential applications in diabetes patients[1].
Succinyladenosine, the metabolic product of dephosphorylation of intracellular adenylosuccinic acid (S-AMP) by cytosolic 5-nucleotidase, is a biochemical marker of adenylosuccinase (ASL) deficiency[1].
CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
2,6-Dimethylhydroquinone is an endogenous metabolite.