Arabinitol, D- is a polyol and its accumulation may cause a neurotoxic effect in human.
3-Oxocholic acid is an oxo-bile acid metabolite and also a major degradation product from cholic by C. perfringens in the intestine. 3-Oxocholic acid is steroid acid found predominantly in bile of mammals[1][2][3].
β-glycosidase-IN-1 (Compound 33) is a piperidine derivative and a β-glycosidase inhibitor. β-glycosidase-IN-1 has hypoglycemic activity[1].
Insulin cattle is a kind of polypeptide hormone that regulates glucose metabolism in pancreatic islet B-cells.
GLP-1(9-36)amide is a major metabolite of glucagon-like peptide-1-(7-36) amide formed by the enzyme dipeptidyl peptidase-4 (DPP-4). GLP-1(9-36)amide acts as an antagonist to the human pancreatic GLP-1 receptor[1][2].
α-Muricholic acid is the most abundant primary bile acid in rodents[1][2].
(24S)-MC 976 is a Vitamin D3 derivative.
Hexapeptide-12isa bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor exhibiting IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
24, 25-Dihydroxy VD2 is a hydroxylated metabolite of Vitamin D2; a synthetic analog of Vitamin D.
ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).IC50 value: 8 nM [1]Target: DGAT-1Oral administration at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels, thus culminating in the nomination of 14 as clinical candidate ABT-046.
cis-Melilotoside, an o-Coumaric acid derivative, shows potent antioxidant activity. cis-Melilotoside has antiprotozoal activity moderately against T. cruzi with an IC50 of 78.2 ug/mL[1][2].
Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.IC50 value: 5.3 nM [1]Target: xanthine oxidoreductasein vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
3α,7α-Dihydroxycoprostanic acid is an endogenous metabolite. 3α,7α-Dihydroxycoprostanic acid, a bile acid, is the precursor to chenodeoxycholic acid[1].
FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes[1].
Diphenyl Phosphate inhibits growth and energy metabolism of zebrafish in a sex-specific manner.
Glibenclamide(Glyburide) is a sulfonylurea compound that modulates insulin production. IC50 value:Target:Sulfonylureas bind to ATP-dependent K+ channels in beta cells of the pancreas, depolarizing them and stimulating the release of Ca2+, which in turn stimulates insulin production. Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim-activated K+ channels in smooth muscle. Binding of Gli to SUR produces the closure of KATP channels and the inhibition of their activity. Glibenclamide is widely used for treatment of type 2-diabetes and it has been signaled as antiproliferative in several tumor cell lines.
VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia[1][2].
Oleic acid-d9 is deuterium labeled Oleic acid. Oleic acid is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator[1][2].
nor-NOHA acetate is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism[1].
YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
Glutathione diethyl ester is a delivery agent for glutathione monoester, and thus for glutathione, in human cells and therefore could serve to decrease oxidative stress and toxicity[1].
Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
Rinderine N-oxide is a pyrrolizidine alkaloid that can be found in R. graeca[1].
Naronapride (ATI-7505) is a potent prokinetic 5-HT4 receptor agonist. Naronapride can be used for gastrointestinal diseases research[1].
Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM. IC50 Value: 3.6±0.2 nM [1]Target: Urotensin Receptor (GPR14)in vitro: Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) [1].in vivo: Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage [2]. Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumulation factor was 1.7 (geometric mean) (95% confidence interval, 1.3 to 2.1).Palosuran was well tolerated [3]. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats [4].Toxicity: Palosuran was well tolerated. No serious adverse events or dose-related adverse events were reported. No treatment-related pattern was detected for vital signs, clinical laboratory parameters, or electrocardiography parameters [5].
Nitrefazole is a 4-nitroimidazole derivative with strong and long lasting inhibition of aldehyde dehydrogenase (ALDH), an enzyme involved in the metabolism of alcohol.
γ-Glu-Gly, a γ-glutamyl dipeptide, is a human lipid metabolite.γ-Glu-Gly has a similar structure to GABA (γ-aminobutyric acid) and can act as an antagonist of excitatory amino acids[1][2][3].
AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.