drugmetabolite

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.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

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.

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

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

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.

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.

Monomethyl fumarate is a potent agonist of GPR109A .

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.

4-Desmethoxy Omeprazole, the active metabolite of Omeprazole, acts as a proton pump inhibitor (PPI) and demonstrates competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM.

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

Hydroxyhexamide ((±)-Hydroxyhexamid) is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agent.

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).