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.

Trimethylamine N-oxide dihydrate (TMANO Dihydrate), a product of the oxidation of trimethylamine, is considered as a protein stabilizer that may serve to counteract urea, the major osmolyte of sharks, skates and rays.

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.

3-Hydroxybutyric acid (Butanoic acid) (or beta-hydroxybutyrate) is a ketone body. Like the other ketone bodies (acetoacetate and acetone), levels of 3-hydroxybutyrate in blood and urine are raised in ketosis. In humans, 3-hydroxybutyrate is synthesized in the liver from acetyl-CoA and can be used as an energy source by the brain when blood glucose is low. Blood levels of 3-hydroxybutyric acid levels may be monitored in diabetic patients to look for diabetic ketoacidosis. Persistent mild hyperketonemia is a common finding in newborns. Ketone bodies serve as an indispensable source of energy for extrahepatic tissues, especially the brain and lung of developing mammals. Another important function of ketone bodies is to provide acetoacetyl-CoA and acetyl-CoA for the synthesis of cholesterol, fatty acids, and complex lipids. During the early postnatal period, acetoacetate (AcAc) and beta-hydroxybutyrate are preferred over glucose as substrates for synthesis of phospholipids and sphingolipids in accord with requirements for brain growth and myelination. Thus, during the first 2 weeks of postnatal development, when the accumulation of cholesterol and phospholipids accelerates, the proportion of ketone bodies incorporated into these lipids increases. On the other hand, an increased proportion of ketone bodies is utilized for cerebroside synthesis during the period of active myelination. In the lung, AcAc serves better than glucose as a precursor for the synthesis of lung phospholipids. The synthesized lipids, particularly dipalmitoylphosphatidylcholine, are incorporated into surfactant, and thus have a potential role in supplying adequate surfactant lipids to maintain lung function during the early days of life (PMID: 3884391 ). 3-Hydroxybutyric acid is found to be associated with fumarase deficiency and medium-chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.

Inosine (NSC-20262) is a purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It has immunomodulatory, neuroprotective, and analgesic properties.

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.

Ecdysone is a major steroid hormone in insects and herbs. Ecdysone triggers mineralocorticoid receptor activation and induces cellular apoptosis. Ecdysone signaling through Ecdysone receptor isoform B1 is required cell autonomously for the muscle death.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Niraparib metabolite M1 (Niraparib carboxylic acid metabolite M1) is the carboxylic acid metabolite of Niraparib. Niraparib is a novel poly (ADP-ribose) polymerase (PARP) inhibitor used in cancer research.

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.

Abemaciclib metabolite M20 (CDK4 6-IN-4) is an active metabolite of Abemaciclib. Abemaciclib metabolite M20 is a selective CDK4 6 inhibitor and can be used for researches on the treatment of cancer.

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.

Niraparib metabolite M1 HCl is the active metabolite of Niraparib, as a novel targeted ADP ribose polymerase (PARP) inhibitor, it can competitively inhibit PARP1 and PARP2 to block the DNA repair mechanism of tumor cells and thus effectively inhibit the growth and proliferation, which is commonly used in the study of ovarian cancer, fallopian tube cancer and primary peritoneal cancer, and is commonly used in the study of ovarian, fallopian tube and primary peritoneal cancers.

Abiraterone Metabolite 1, a 5β-reduced derivative of abiraterone, acts by inhibiting CYP17A1, thereby blocking androgen synthesis and extending survival in prostate cancer patients.

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

Tetrabenazine Metabolite ((-)-β-HTBZ), a vesicles monoamine transporter 2 (VMAT2) inhibitor, is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite has a high affinity for VMAT2 with a Ki of 13.4 nM. Tetrabenazine Metabolite is often used to study chorea associated with Huntington's disease and other hyperactivity disorders.

Ticagrelor metabolite M5 (T437700) is a metabolite of Ticagrelor, the first reversible oral antagonist of P2Y12 receptor. Compared to Clopidogrel, Ticagrelor has faster and more consistent inhibition on ADP-receptors. Ticagrelor is used in the treatment of acute coronary syndromes (ACS).

Norgestimate metabolite Norelgestromin (17-Deacylnorgestimate) is one of the active metabolites of norgestimate.It is a steroidal progestin used in contraceptive patches, where it is combined with the estrogen ethinyl estradiol.

Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 , as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.

Deutetrabenazine metabolite M4 is believed to be related to its effect as a reversible depletion of monoamines from nerve terminals. The major circulating metabolites of Deutetrabenazine, are reversible inhibitors of VMAT2, resulting in decreased uptake

Nicardipine pyridine metabolite II is a biaoctive chemical.

Para-Naphthol Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI),is a metabolite of Duloxetine.