drug metabolite

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.

4-Hydroxymephenytoin ((+ -)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

LGE-899 (Sonidegib metabolite M48) is a main metabolite of Sonidegib which is an inhibitor of the hedgehog pathway. The Tmax of LGE-899(60 h) is much longer than Sonidegib.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of atorvastatin calcium salt, a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).

Isonicotinic acid, a metabolite of isoniazid and a useful isomer of nicotinic acid, is formed from isoniazid by hydrazinolysis and can be catalyzed by cytochrome P450 enzymes, such as CYP2C.

Ampyrone (4-Aminoantipyrine) is a reagent for glucose determination in the presence of peroxidase and phenol.

Clofibric acid (Chlorofibrinic acid) is an antilipemic agent that is the biologically active metabolite of CLOFIBRATE.

Monobutyl phthalate, the main metabolite of dibutyl phthalate, is an embryotoxin with antiandrogenic properties.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate) is the ethyl ester of p-Coumaric acid. p-Coumaric Acid is a common dietary polyphenol and also a potent immunosuppressive agent in treating autoimmune inflammatory diseases like rheumatoid arthritis.

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.

3-Methoxytyramine hydrochloride (3-O-methyl Dopamine hydrochloride) is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1). 3-methoxytyramine can be found primarily in human brain and most tissues tissues; and in blood, cerebrospinal fluid (csf) or urine. Within a cell, 3-methoxytyramine is primarily located in the cytoplasm.

Tulipalin A (α-methylene-γ-butyrolactone) (2-Methylenebutyrolactone) which has some phytotoxicity is a natural compound extracted from Tulipa gesneriana.

Mycophenolate Mofetil (TM-MMF), an immunosuppressive agent, is the 2-morpholinoethyl ester of mycophenolic acid (MPA), and an inhibitor of inosine monophosphate dehydrogenase (IMPDH).

4-(4-Amino-3-fluorophenoxy)-N-methylpicolinamide is an aromatic enigma that is is a metabolite of the antitumor drug rafenil.

16α-Hydroxyprednisolone is a stereoselective metabolite of the [22(R)] epimer of the glucocorticoid budesonide.

Homovanillyl alcohol, a biological metabolite of Hydroxytyrosol, is a phenolic compound found in virgin olive oil (VOO) and wine. It exhibits high scavenging activities, protects red blood cells from hemolysis in a dose-dependent manner, and has a protective effect on cardiovascular disease and total mortality.

meta-Fexofenadine (meta-MDL-16455) is an isomer of Fexofenadine.

p,p'-DDE (p,p'-dichlorodiphenyldichloroethylene) is a metabolite and degradation product of the organochlorine pesticide DDT

4-Methylamino antipyrine, an active metabolite of Metamizole, a pyrazolone non-steroidal anti-inflammatory drug (NSAID) that inhibits COX, possesses analgesic, antipyretic, and relatively weak anti-inflammatory properties.

Regorafénib N-oxyde M2 is an active metabolite of Regorafenib, a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, RET, Kit, and Raf-1 (IC50s: 13/4.2/46, 1.5, 22, 7, and 2.5 nM).

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).