7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level[1].
Gancaonin L is an isoflavone, that can be isolated from Glycyrrhiza glabra roots. Gancaonin L exhibits significant PPAR-γ ligand-binding activity. Gancaonin L can be used for anti-diabetes and anti-obesity research[1].
(R)-Pantetheine is the biosynthetic precursor to CoA.(R)-Pantetheine and its corresponding disulfide pantethine, play a key role in metabolism as a building block of coenzyme A (CoA)[1].
Indole-3-methanamine is a potential biomarker for the consumption of these foods such as barley, cereals, and cereal product[1].
SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM)[1][2].
A potent, selective, CNS-penetrant P2X7 antagonist with pKi of 9.1 and 7.9 for rat and huamn P2X7 channel, respectively; does not block calcium flux via human P2X1, P2X2, P2X3, P2X2/P2X3, and P2X4 at 10 uM; attenuates both ATP- and Bz-ATP-induced currents from hP2X7-1321N1 cells with similar potencies (pEC50=7.0), blocks the release of IL-1β induced by Bz-ATP in freely moving rat brain, also increases serotonin levels; attenuates amphetamine-induced hyperactivity in vivo.
6-Methyluracil (Pseudothymine), a metabolite of Uracil, can be used as an indicator of acetoacetyl-CoA (AACoA) accumulation. 6-Methyluracil exhibits antiradiation effect in vivo[1][2].
Palmitic acid-1,2,3,4-13C4 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
MBX 102 is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
5-Methyltetrahydrofolic acid is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid[1].
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes[1].
Enterostatin, human, mouse, rat is a pentapeptide that reduces fat intake.
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications.
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
Ficusonolide has significant antidiabetic activity with a possible mechanism of interaction with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.
L17E, an endosomolytic peptide, is a cationic amphiphilic peptide with specific membrane lytic activity for late endosomes (LEs). L17E diminishes the TS5-p45 induced apoptosis in a dose-dependent manner. L17E is endocytosed into cells and trafficked to LEs. Within the acidic environment of LEs, L17E perturbs and lyses the LE membrane, leading to disruption of LE membrane and release of LE content to the cytosol. L17E is used to investigate the role of the endosomal protein trafficking pathway[1].
Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.
Arteanoflavone, a natural compound that can be isolated from A. iwayomogi, possess inhibitory activities on AGEs formation[1].
2-Acetyl-3-ethylpyrazine is an endogenous metabolite.
Amylin (8-37) (human) (hIAPP (8-37)) is a 8-37 fragment of human islet amyloid polypeptide (IAPP). The duplex folding structure in the Amylin (8-37) (human) assembly has a hairpin structure[1].
SLU-PP-915 is an agonist of ERR. SLU-PP-915 has an EC50 value of approximately 400 nM for ERRα, ERRβ, and ERRγ. SLU-PP-915 has potential application in maintaining oxidative metabolism and heart failure[1][2][3].
Adomeglivant is a potent and selective glucagon receptor antagonist that is used in clinical trial for type 2 diabetes mellitus.
Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) is a potent dual inhibitor of pancreatic lipase (PL) and human carboxylesterase 1A (hCES1A) with IC50 values of 2.13 µM and 0.055 µM against PL and hCES1A[1].
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects[1][2][3][4].
Tetradecyl-β-D-maltoside is an absorption enhancer which can increase the nasal absorption of regular human insulin or the fast acting insulin analog lyspro-insulin[1].
16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy[1].
KAT681 is a liver-selective thyromimetic.
Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
Ganoderal A, an oxygenated sterol from G. lucidum, is a cholesterol synthesis inhibitor[1].
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia[1].