PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
Pegylated synthetic human c-peptide retains bioactivity comparable to that of natural (i.e. non-polyethylene glycolated) C-peptides and has a prolonged circulating residence time in plasma for use in diabetic peripheral neuropathy studies[1].
α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia[1].
SCH 39166 hydrobromide (SCH391660) is potent and selective antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. SCH 39166 hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). SCH 39166 hydrobromide can be used for the research of schizophrenia, cocaine addition, and obesity[1].
Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877)[1][2]. Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM[3].
GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9. GW1100 acts as a GPR40 inverse agonist.
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader[1].
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.IC50 value: 5.6/7.9 uM ( recombinant mouse/ human GPR119) [1]Target: GPR119 agonistSystemic administration of PSN632408 (30 mg/kgintraperitoneally) suppresses food intake, reduces weight gain, and white adipose tissue deposition in rats. GPR119 (previously designated SNORF25) is an orphan G protein-coupled receptor expressed predominantly in the pancreas and gastrointestinal tract in humans and in the brain, pancreas, and gastrointestinal tract in rodents. It mediates a reduction in food intake and body weight gain in rats upon treatment with oleoyl ethanolamide (OEA), an endogenous, potent agonist for PPARα. These data suggest that PSN632408 may be useful as a therapeutic agent for the treatment of obesity.
Adenosine is a nucleoside composed of a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond.Target: Nucleoside antimetabolite/analogAdenosine plays an important role in biochemical processes, such as energy transfer — as adenosine triphosphate (ATP) and adenosine diphosphate (ADP) — as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter, believed to play a role in promoting sleep and suppressing arousal. Adenosine also plays a role in regulation of blood flow to various organs through vasodilation.Adenosine is an endogenous purine nucleoside that modulates many physiological processes. Cellular signaling by adenosine occurs through four known adenosine receptor subtypes. Extracellular adenosine concentrations from normal cells are approximately 300 nM; however, in response to cellular damage (e.g. in inflammatory or ischemic tissue), these concentrations are quickly elevated (600–1,200 nM). Thus, in regard to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia, and seizure activity. Activation of A2A receptors produces a constellation of responses that in general can be classified as anti-inflammatory.
Glycohyodeoxycholic acid is a major metabolite of Hyodeoxycholic acid in humans. Glycohyodeoxycholic acid has preventative effects on gallstone formation[1][2].
Muraglitazar is a PPAR α/γ dual agonist for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα (EC50 = 320 nM) and PPARγ(EC50 = 110 nM)[1].
Dextranase, glucan hydrolase, is often used in biochemical research. Dextranase can catalyze the hydrolysis of α-(1,6)-glucosidic bonds in dextran, and has a wide range of applications, such as food processing, sugar modification, drug preparation, and medicine for enhancing the activity of endocarditis antibiotics wait[1].
Sphingolipid ceramide N-deacylase (SCDase) cleaves the N-acyl linkage between fatty acids and sphingosine bases in various glycosphingolipids. Sphingolipid ceramide N-deacylase catalyzes glycosphingolipids to lysoglycosphingolipids[1].
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
L-Tryptophan-15N2 (Tryptophan-15N2) is the 15N-labeled L-Tryptophan. L-Tryptophan (Tryptophan) is an essential amino acid that is the precursor of serotonin, melatonin, and vitamin B3[1].
SH-BC-893 is a water-soluble, orally bioavailable synthetic sphingolipid that triggers nutrient transporter internalization and also blocks lysosome-dependent nutrient generation pathways in cancer cells, activates protein phosphatase 2A (PP2A), leading to mislocalization of the lipid kinase PIKfyve; selectively kills cells expressing an activated form of the anabolic oncogene Ras in vitro and in vivo.
β-Casomorphin, human is an opioid peptide, acts as an agonist of opioid receptor.
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM)[1].
VD3-D6(Vitamin D3-26,26,26,27,27,27-d6) is the deuterated form of Vitamin D3; tools for determination of Vitamin D3 metabolites in human serum.
Pioglitazone is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
Petunidin-3-O-glucoside chloride is a flavonoid isolated from Phaseolus vulgaris L. seed, has antioxidant activity[1]
S-Allyl-L-cysteine, one of the organosulfur compounds found in AGE, possess various biological effects including neurotrophic activity, anti-cancer activity, anti-inflammatory activity.
Kojibiose, an orally active prebiotic disaccharide, can specifically inhibit the activity of α-glucosidase I. kojibiose is a proliferation factor for Bifidobacterium, lactic acid bacteria, and eubacteria. kojibiose is a low-calorie sweetener capable of increasing the absorption of iron. Kojibiose exhibits antitoxic activity. Kojibiose reduces hepatic expression of inflammatory markers in vivo[1][2].
D-Glucose-18O is the 18O 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
MK-0159 (compound 37) is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD+ (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart[1].
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity[1].
Fmoc-leucine-13C6,15N is a 15N-labeled and 13C-labled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity
Allolithocholic acid is a steroid acid could found in normal serum and feces. Allolithocholic acid facilitates excretion, absorption, and transport of fats and sterols in the intestine and liver[1].
α-Glucosidase-IN-23 is an orally active α-Glucosidase inhibitor. α-Glucosidase-IN-23 decreases blood glucose by a-glucosidase inhibition with an IC50 value of 4.48 μM. α-Glucosidase-IN-23 can be used for the research of diabetes[1].
Ascorbate oxidase, also known as vitamin C oxidase, is a REDOX enzyme involved in the regulation of extracellular matrix. Ascorbate oxidase catalyzes the reaction of ascorbic acid and oxygen to produce dehydroascorbic acid[1][2].