Cyclohexaneacetic acid is an endogenous metabolite.
Glucarpidase is an enzyme that inactivates methotrexate. Glucarpidase can be used for renal dysfunction diseases research[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].
AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
L-Alanine-1-13C,15N (L-2-Aminopropionic acid-1-13C,15N) is the 13C- and 15N-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
SCH-900271 is an orally active, potent nicotinic acid receptor (NAR) agonist with an EC50 of 2 nM in the hu-GPR109a assay. SCH-900271 exhibits dose-dependent inhibition of plasma free fatty acid (FFA). SCH-900271 has an improved therapeutic window to flushing[1].
Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
Etomoxir ((R)-(+)-Etomoxir) is a potent inhibitor of carnitine palmitoyltransferase-I (CPT-1).
Tegaserod is a serotonin receptor 4 agonist (HTR4) used in the treatment of irritable bowel syndrome (IBS). Anti-tumor activity[1].
MGAT2-IN-2 is a potent and selective acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 3.4 nM.
OSBPL7-IN-1 is an orally active oxysterol binding protein like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes an increase of ABCA1 at the plasma membrane without affecting mRNA expression[1].
Lovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM[1].
RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively[1].
Rinderine N-oxide is a pyrrolizidine alkaloid that can be found in R. graeca[1].
Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs)[1].
Epoetin beta (rhEPO) is a recombinant form of erythropoietin. Epoetin beta is responsible for the maintenance of erythropoiesis and can be used for anaemia research[1].
Alirocumab (REGN 727) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9). Alirocumab specifically binds PCSK9, a down regulator of liver low-density lipoprotein (LDL)-receptors, thereby increasing the ability of the liver to bind LDL-cholesterol (LDL-C) and reducing levels of LDL-C in blood. Alirocumab can be used for the research of hypercholesterolemia[1].
Imirestat (AL 1576) is an aldose reductase inhibitor, used for the treatment of diabetes.
GDP-L-fucose is a nucleotide sugar that is a key substrate for the biosynthesis of fucose oligosaccharides, providing the fucose moiety for the oligosaccharides.The formation of GDP-L-fucose occurs through two pathways, the major ab initio metabolic pathway and the minor remedial metabolic pathway[1].
L-Glutamine-15N2 (L-Glutamic acid 5-amide-15N2) is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].
Naronapride (ATI-7505) is a potent prokinetic 5-HT4 receptor agonist. Naronapride can be used for gastrointestinal diseases research[1].
Tripeptide-41(CG-Lipoxyn)isa bioactive peptide withreduce fat accumulationeffect and has been reported used as a cosmetic ingredient[1].
(Rac)-3-Hydroxyphenylglycine is an phosphoinositide hydrolysis agonist[1]. ACPD: I-aminocyclopcntane-1,3-dicarboxylic acid.
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].
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL)[1].
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity[1][2][3][4][5].
KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.
Nitrefazole is a 4-nitroimidazole derivative with strong and long lasting inhibition of aldehyde dehydrogenase (ALDH), an enzyme involved in the metabolism of alcohol.