Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4].
Xenopsin-Related Peptide 2 (XP-2) is an avian counterpart to amphibian Xenopsin (HY-P0253). Xenopsin-Related Peptide 2 displays abilities to release histamine from isolated rat mast cells and is as effective as synthetic Bradykinin (HY-P0206)[1].
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].
BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells[1].
1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA) is an endogenous metabolite. 1-Palmitoyl-sn-glycerol 3-phosphate can be used for the research of non‐alcoholic fatty liver disease[1].
UAMC-3203 is a potent and selective Ferroptosis inhibitor with an IC50 of 12 nM.
GJ103 is a read-through compound that can induce read through of premature stop codons. GJ103 has potential for the research of genetic disorders caused by nonsense mutations[1].
Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate is a mouse-modeling drug that can induce Mallory body (MB) formation. MBs reached maximum concentration on day 5 of refeeding. Liver cell regeneration increased on the third day of refeeding[1].
Isovaleric acid-13C is the 13C labeled Isovaleric acid. Isovaleric acid is a natural fatty acid and known to effect on neonatal death and possible Jamaican vomiting sickness in human.
MHY908 is a potent dual agonist of PPARα and PPARγ[1]. MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity[2].
Rimonabant hydrochloride is a cannabinoid receptor (CB) antagonist which binds selectively to CB1 with a Ki of 2 nM.
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13±3 nM.
Cockroach Myoactive Peptide II (Pea-CAH-II) is a cockroach neuropeptide. Cockroach Myoactive Peptide II is a member of the adipokinetic hormone/red pigment concentrating hormone (AKH/RPCH) family. Cockroach Myoactive Peptide II can be used for the research of metabolic functions of insect body[1].
Febuxostat (TEI 6720) sodium is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat sodium has the potential for the research of hyperuricemia and gout[1][2][3].
1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine-d62 is deuterium labeled 1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine. 1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine is an endogenous metabolite.
Neotheaflavin, from black tea, inhibits pancreatic lipase[1].
Sorbinil, is an Aldose reductase inhibitor (ARI).Sorbinil plays therapeutic role in treating diabetes and diabetic complications, decreases AR activity and inhibits polyol pathway, it to be found comparatively safer than other ARIs for human use[1].
Atorvastatin methyl ester (Compound 2a) is a methyl esterified derivative of Atorvastatin. Atorvastatin methyl ester inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin[1].
CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
Acyl coenzyme A synthetase (ACS), namely acetyl coenzyme A synthetase, is often used in biochemical research. Acyl coenzyme A synthetase can catalyze the activation of fatty acids by coenzyme A through a two-step thioesterification reaction to produce acyl coenzyme A, and then participate in a variety of anabolic and catabolic lipid metabolism pathways, and participate in the TCA cycle in aerobic respiration[1].
Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
Guaifenesin is an expectorant that also has some muscle relaxing action.Target: OthersGuaifenesin is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. It also stimulates the flow of respiratory tract secretions, allowing ciliary movement to carry the loosened secretions upward toward the pharynx. Thus, it may increase the efficiency of the cough reflex and facilitate removal of the secretions; however, objective evidence for this is limited and conflicting [1].
BI 01383298 is a potent inhibitor of the sodium-citrate co-transporter (SLC13A5) that is highly expressed in the liver[1].
PTP1B-IN-3 is a potent and selective PTP1B inhibitor with IC50s of 120 nM (PTP1B) and 120 nM (TCPTP), respectively.
sn-Glycerol 3-phosphate biscyclohexylammonium salt is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.
4'-Trifluoromethyl-2-biphenyl carboxylic acid is an orally active hypolipidemic agent[1].
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity[1].
1-Hydroxyoctadecane-d2 is the deuterium labeled 1-Hydroxyoctadecane[1]. 1-Hydroxyoctadecane is an endogenous metabolite.
Tris(dihydrocaffeoyl)spermidine is an active compound. Tris(dihydrocaffeoyl)spermidine can be isolated from potato (Solanum tuberosum) tubers. Tris(dihydrocaffeoyl)spermidine can be used for the research of metabolism[1].
alpha-1,3-Galactosyltransferase(GTB) (alpha3GT) catalyzes the synthesis of the xenoantigen or α-galactose (α-Gal) epitope. alpha-1,3-Galactosyltransferase(GTB) transfers galactose from UDP-Gal to type 1 or type 2, αFuc1→2βGal-R (H)-terminating acceptors[1].