metabolite

GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral bioavailability.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

(R)-Lisofylline ((R)-Lisophylline) is an inhibitor of lysophosphatidic acid acyltransferase (IC₅₀ = 0.6 µM) that interrupts IL-12 signaling-mediated STAT4 activation, making it useful for studies on the treatment of type 1 diabetes and autoimmune disorders.

Paliperidone (9-hydroxyrisperidone)(Invega) is used as an atypical antipsychotic. It applies to the acute and maintenance treatment of schizophrenia. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone.

Prasugrel (CS-747) is a piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.

Inosine (NSC-20262), an endogenous purine nucleoside produced by the catabolism of adenosine, is an agonist of adenosine receptors A1R and A2AR. Inosine has anti-inflammatory, immunomodulatory, antinociceptive and neuroprotective effects.

1-Aminohydantoin hydrochloride is a significant metabolite of furantoin in animal tissues. It binds covalently to tissue proteins, is released under slightly acidic conditions, and can be detected by derivatization with 2-nitrobenzaldehyde forming a nitrophenyl derivative of AHD. It is used in assays to determine veterinary drug residues in meat and milk.

Monomethyl fumarate is a potent agonist of GPR109A .

Octadecanedioic acid is an endogenous metabolite, is a long-chain dicarboxylic acid.

Nortriptyline hydrochloride (ELF-101 hydrochloride) is a metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.

Hexadecanal (Palmitaldehyde) is a free fatty aldehyde found in animals.

Rabeprazole Sulfide (Rabeprazole Related Compound E) is an antiulcer drug in the class of proton pump inhibitors.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

Usnic Acid (Usniacin) is an antimicrobial, antitumor and enzyme inhibiting agent shown to uncouple oxidative phosphorylation in mouse-liver mitochondria. Usnic acid induces necrosis in certain cells.

N-acetyl Sulfamethoxazole is a metabolite of sulfamethoxazole, an antibiotic with antiviral activity, that can be detected in urine.

Dimetridazole is a nitroimidazole-based compound with antibacterial and anticoccidial activity. It was once widely used in the treatment of parasitic infections in poultry, cattle, swine and farmed fish until suspected to be carcinogenic and mutagenic to humans. Hydroxy dimetridazole is a metabolite of dimetridazole that may be useful for identifying this nitroimidazole in various agricultural samples through liquid chromatography-tandem mass spectrometry and other methods.

D-Threonine (H-D-Thr-OH) is a metabolite of Saccharomyces cerevisiae.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC₅₀ of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

Linoleic acid (9,12-octadecadienoic acid) is a naturally occurring polyunsaturated fatty acid found in animal and vegetable oils. Linoleic acid is an essential fatty acid that is part of membrane phospholipids.

L-Tartaric acid ((2R,3R)-(+)-Tartaric acid) occurs naturally in many plants, particularly grapes and tamarinds, and is one of the main acids found in wine. It is used as an antioxidant. Salts of tartaric acid are known as tartrates. L-Tartaric acid is a muscle toxin, which works by inhibiting the production of malic acid, and in high doses causes paralysis and death.

Trimethylamine N-oxide dihydrate (TMANO dihydrate) is a gut microbiota-dependent metabolite derived from dietary choline and other trimethylamine-containing nutrients. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation and cardiac fibrosis via the TGF-β/Smad2 signaling pathway. TMANO dihydrate can be used to establish models of cardiac hypertrophy and cardiac fibrosis.

H-Tyr(3-I)-OH (3-Iodo-L-tyrosine) is an inhibitor of tyrosine hydroxylase (Ki = 0.39 M) and an intermediate in the synthesis of thyroid hormones

Desfesoterodine (5-HMT) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

3-(3-Hydroxyphenyl)propionic Acid (m-Hydroxyphenylpropionic acid) is one of the major metabolites of ingested caffeic acid.it inhibited osteoclastogenesis and bone osteoclastic resorptive activity.