1-Palmitoyl-2-hydroxy-sn-glycero-3-PE is a lysophospholipid acyl acceptor. 1-Palmitoyl-2-hydroxy-sn-glycero-3-PE is used as a structure-related lipid control[1].
Malic enzyme inhibitor ME1 (ME1) is a multifunctional protein involved in glycolysis, the citric acid cycle, NADPH production, glutamine metabolism, and lipogenesis[1]. Malic enzyme inhibitor ME1 regulates one of the main pathways that provide nicotinamide adenine dinucleotide phosphate (NADPH), which is essential for cancer cell growth through maintenance of redox balance and biosynthesis processes in the cytoplasm. Malic enzyme inhibitor ME1 disrupts metabolism in cancer cells and inhibits cancer cell growth by inducing senescence or apoptosis [2].
D-Glucose-13C-3 is the 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα[1][2].
Magnoloside B is an α-glucosidase inhibitor (IC50=0.69 mM), which can be obtained from Magnolia officinalis stem bark. Magnoloside B shows moderate inhibitory activity against MGC-803 and HepG2 cells. Magnoloside B has the potential to study cancer and diabetes[1].
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a Kd of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes[1].
2-Methylbenzaldehyde is an endogenous metabolite.
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death[1][2][3].
Hexokinase is a glycolytic enzyme hexokinase that is inhibited by n-acetylglucosamine. Inhibition of hexokinase by n-acetylglucosamine leads to its separation from the mitochondrial outer membrane, resulting in activation of NLRP3 inflammasome[1].
23,25-Dihydroxy-24-oxovitamin D3 is a major metabolite of 24(R),25-Dihydroxyvitamin D3. 23,25-Dihydroxy-24-oxovitamin D3 can be used for the research of metabolic diseases[1].
LX2761 is chemically stable and potent inhibitor against sodium-dependent glucose cotransporter 1 (SGLT1) and SGLT2 in vitro with IC50s of 2.2 nM and 2.7nM for hSGLT1 and hSGLT2, but displays specific SGLT1 inhibition in the gastrointestinal (GI) tract[1].
Citric acid trisodium is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium causes renal toxicity in mice[1][2][3].
Mitiglinide calcium hydrate is a drug for the treatment of type 2 diabetes; it is a highly selective KATP channel antagonist. IC50 value:Target: KATP channel
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity[1].
α-L-Fucosidase (EC 3.2.1.51) is an enzyme that catalyzes the chemical reaction. Serum activity of α-L-fucosidase, a lysosomal enzyme present in all mammalian cells, has been proposed as a marker of hepatocellular carcinoma (HCC)[1].
BDC2.5 mimotope 1040-31 is a strong agonistic peptide for diabetogenic T cell clone BDC2.5, and the 1040-31 peptide is specific for BDC 2.5 TCR Tg+ T cells[1][2].
Amaroswerin is a bioactive secoiridoid glucoside from Swertia mussotii. Amaroswerin has anti-inflammatory, antidiabetic, antiviral, anticholinergic and immunomodulatory activities. Amaroswerin inhibits NO release with an IC50 value of 5.42 μg/mL in RAW264.7 cells[1].
PPARγ agonist 8 is an agonist of PPARγ. PPARγ agonist 8 induces peroxisome proliferator response element (PPRE)-luciferase activity with an EC50 of 0.2 μM[1].
Galactose 1-phosphate-13C-1 potassium is the 13C labeled Galactose 1-phosphate Potassium salt. Galactose 1-phosphate Potassium salt is is an intermediate in the galactose metabolism and nucleotide sug[1][2].
JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats[1].
Malate dehydrogenase catalyzes the mutual conversion of oxaloacetate and malate, and is associated with the oxidation/reduction of dinucleotide coenzymes[1].
10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism[1].
Cimicifugoside H-1, a cyclolanostanol xyloside, is a major constituent of C. foetida L. extract. Cimicifugoside H-1 inhibits bone resorption and ovariectomy-induced bone loss[1][2][3].
Microsomal aminopeptidase (microsomal aminoptidase) was first reported from C. elegans. The Microsomal aminopeptidase is beneficial for the development of molecular vaccines against parasitic nematodes[1].
Retinyl-β-D-glucoside is a naturally occurring and biologically active metabolites of vitamin A, which are found in fish and mammals.IC50 Value: Target: in vitro: Retinyl beta-D-glucoside is a substrate for two broad-specificity mammalian beta-glucosidases, namely the cytosolic and membrane-associated beta-glucosidases of guinea pig liver. However, retinyl beta-D-glucoside is not hydrolysed by placental glucocerebrosidase [1].in vivo: Depending on the mode of administration, retinyl beta-glucose, which is soluble in water, showed 67-100% of the growth-promoting activity of retinyl acetate in vitamin A-deficient rats. In metabolic studies on vitamin A-deficient rats, retinyl beta-glucose was rapidly hydrolyzed to retinol [2].
L-Gulose, the putative furanose form of L-sorbosone, is an L-hexose sugar and an intermediate in the biosynthesis of L-Ascorbate (vitamin C)[1].
6β-Hydroxyipolamiide can be isolated from the methanolic extract of S. jamaicensis leaves. 6β-Hydroxyipolamiide has α-glucosidase inhibitory activity with an IC50 of 539.17 μg/mL[1].
AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).IC50 value: 80 nM [1]Target: DGAT1in vitro: Plasma AZD7687 exposure was measured repeatedly. Postprandial serum TAG excursion was measured during 8 h after a standardized mixed meal with fat energy content of 60% (SMM 60%; five cohorts, 1-20 mg), before (baseline) and after dosing, to assess effects on gut DGAT1 activity. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship [2].in vivo: Multiple doses of AZD7687 (1, 2.5, 5, 10 and 20 mg/day, n=6 or n=12 for each) or placebo (n=20) were administered for 1 week. Dose-dependent reductions in postprandial serum TAG were demonstrated with AZD7687 doses ≥5mg compared with placebo (p<0.01). Significant (p<0.001) increases in plasma GLP-1 and PYY levels were seen at these doses, but no clear effect on gastric emptying was demonstrated at the end of treatment. With AZD7687 doses >5 mg/day, gastrointestinal (GI) side effects increased; 11/18 of these participants discontinued treatment owing to diarrhoea [3].