metabolized

Broflanilide is metabolized to desmethyl-broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin GABA receptor and inhibits S. litura RDL GABAR (IC50: 1.3 nM).

GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which penetrates the skin and is metabolized in the epithelium to an active nucleoside triphosphate analogue.GS-9191 has antiproliferative activity and reduces the size of papillomas in a dose-related manner.GS-9191 may be useful in the treatment of HPV-induced lesions.

L-Histidine (L-(-)-Histidine) is a semi-essential amino acid (children should obtain it from food) needed in humans for growth and tissue repair, L-Histidine is important for maintenance of myelin sheaths that protect nerve cells and is metabolized to the neurotransmitter histamine. Histamines play many roles in immunity, gastric secretion, and sexual functions. L-Histidine is also required for blood cell manufacture and protects tissues against damage caused by radiation and heavy metals.

Methyldopa (MK-351), an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive medicine, is served as an antihypertensive or sympatholytic.

Diammonium Glycyrrhizinate (Glycyrrhizin) , an extensively used anti-inflammatory agent, is isolated from the licorice root. It is metabolized to glycyrrhetinic acid, which inhibits 11-β-hydroxysteroid dehydrogenase and other enzymes involved in the metabolism of corticosteroids. Therefore, glycyrrhizic acid, the main and sweet component of licorice, has been studied for its ability to cause hypermineralocorticoidism with potassium loss and sodium retention, edema, increased blood pressure, as well as inhibited the renin-angiotensin-aldosterone system.

2-Phenylethylamine hydrochloride (benzeneethanamine hydrochloride) acts as neuromodulator in the central nervous system. It stimulates the release of norepinephrine and dopamine and is metabolized by monoamine oxidases as well as other enzymes.

Oxalic acid is a strong dicarboxylic acid occurring in many plants. Oxalic acid is produced in the body by metabolism of glyoxylic acid or ascorbic acid.

Oxalic acid dihydrate (Ethanedioic acid dihydrate) is a strong dicarboxylic acid occurring in many plants and vegetables. It is produced in the body by metabolism of glyoxylic acid or ascorbic acid. It is not metabolized but excreted in the urine. It is used as an analytical reagent and general reducing agent.

Methyldopa hydrate (MK-351 hydrate) is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension. It inhibits the sympathetic nervous system, decreases production of dopamine, norepinephrine, and epinephrine, and exhibits NO-dependent sedative activity.

Terfenadine ((±)-Terfenadine) is a prodrug metabolized by intestinal CYP3A4 into fexofenadine, an active selective histamine H1-receptor antagonist that possesses antihistaminic and non-sedative effects.

Potassium 1-carboxyvinyl hydrogenphosphate (PEP-K) is involved in glycolysis and gluconeogeneis. In glycolysis, PEP is metabolized by Pyruvate Kinase to yield pyruvate. In plants, PEP is involved in the formation of aromatic amino acids as well as in the carbon fixation pathway.

Tinidazole (CP12574)a is a 5-nitroimidazole derivative with the antiprotozoal property. Although the mechanism of action has not been fully elucidated, it has been suggested that tinidazole is metabolized and yields nitrite anions and metronidazole. Metronidazole's nitro group, in turn, is reduced via the parasite ferredoxin, thereby generating a series of free nitro radicals including nitro anions. Toxicity is achieved via depletion of sulfhydryl groups and DNA strand breaks with multiple hits having an additive effect and ultimately leading to cell death.

Cholestenone is an intermediate oxidation product of cholesterol that is metabolized primarily in the liver. It can cause long-term defects in cell function. It is highly mobile in membranes and affects cholesterol turnover and efflux.

Capecitabine (Capecitibine) is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.

AG 045572 is a potent GnRH receptor antagonist that inhibits the GnRH receptor in humans and rats with Ki values of 6.0 nM and 3.8 nM, respectively.AG 045572 is metabolized by CYP3A and inhibits testosterone.

Methyl-a-L-fucopyranoside (Methyl alpha-L-fucopyranoside) is a rhizobial lectin inhibitor that is not metabolized by the fungus and prevents the biocontrol agent Trichoderma reesei from coiling around the rhizobial mycelium.Methyl-a-L-fucopyranoside is inhibitory to Lectin PLL3, LECB and BAMBL.

Calcifediol (U 32070E) is a naturally occurring product that is metabolized in the liver from vitamin D3, a VDR ligand. Calcifediol is indicated for use as a vitamin supplement for all patients with vitamin D deficiency.

Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

Eleutheroside E has anti-inflammatory effects by inhibiting NF-κB activities. Eleutheroside E significantly decreases the inflammatory cell infiltration, pannus formation, cartilage damage, bone erosion of CIA mice, the generation of TNF-α and IL-6, the m

Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

Lofepramine (Leo 640) is a potent tricyclic antidepressant that is extensively metabolized to desipramine. It inhibits the serotonin and norepinephrine transporters by inhibiting neurons with Kd values of 70 and 5.4 nM, respectively, with weak antagonism of serotonin, histamine and muscarinic receptors.

Cholestenone is an intermediate oxidation product of cholesterol that is metabolized primarily in the liver. It can cause long-term defects in cell function. It is highly mobile in membranes and affects cholesterol turnover and efflux.

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2 M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

Dehydroaripiprazole (DM-14857) is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.

13(S)-HpOTrE is a monohydroperoxy polyunsaturated fatty acid produced in soybeans by the action of soybean LO-2 on esterified α-linolenic acid.[1] Incubation of soybean seedling biomembranes with soybean LO-2 catalyzes the formation of both 9- and 13-HpOTrE in a molar ratio of 10:1.1 In plants, 13(S)-HpOTrE can be metabolized by the hydroperoxide lyase pathway producing aldehyde and oxoacid fragments, or by the hydroperoxide dehydratase pathway producing jasmonic acid.[2],[3],[4] Treatment of tomato leaves with 13-HpOTrE causes induction of proteinase inhibitors, simulating the normal response to wounding.5 This data suggests that in plants 13(S)-HpOTrE may participate in a lipid-based signalling system initiated by insect and pathogen attack.

6β-hydroxy Dexamethasone is a metabolite of dexamethasone that is more hydrophilic than the parent compound. Dexamethasone is metabolized by CYP3A4; therefore, quantification of the dexamethasone metabolites, 6α- and 6β-hydroxy dexamethasone, can be used to determine CYP3A4 enzyme activity in humans., The formation of 6-hydroxy dexamethasone metabolites is species-specific, with hamsters producing the highest amount. In rats, dexamethasone hydroxylation is sex-specific, with male rats producing metabolites in similar ratios to humans and female rats producing fewer hydroxylated metabolites than male rats.

Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver, assisting BOS pharmacologically with 10%-20% activity retention.

Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants. Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid . Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 μM). It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress. Jacaric acid is metabolized in vivo to conjugated linoleic acid , which is also cytotoxic to cancer cells. Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 μM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.

9AzNue5Ac is a Neu5Ac analog that is metabolized in living cells and in mice.9AzNue5Ac binds to salivary glycans.

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.

Nitrated unsaturated fatty acids, such as 10- and 12-nitrolinoleate , cholesteryl nitrolinoleate, and nitrohydroxylinoleate, represent a new class of endogenous lipid-derived signalling molecules. LNO2 isomers serve as potent endogenous ligands for PPARγ and can also decompose or be metabolized to release nitric oxide. 9-Nitrooleate is one of two regioisomers of nitrooleate, the other being 10-nitrooleate (OA-NO2; used for the mixture of isomers), which are formed by nitration of oleic acid in approximately equal proportions in vivo. Peroxynitrite, acidified nitrite, and myeloperoxidase in the presence of H2O2 and nitrite, all mediate the nitration of oleic acid. OA-NO2 is found in human plasma as the free acid and esterified in phospholipids at concentrations of 619 ± 52 nM and 302 ± 369 nM, respectively. OA-NO2 activates PPARγ approximately 7-fold at a concentration of 1 μM and effectively promotes differentiation 3T3-L1 preadipocytes to adipocytes at 3 μM.

(±)4(5)-EpDPA methyl ester is a derivative of (±)4(5)-EpDPA which is stable enough to ship and handle routinely. The active free acid can be regenerated from the methyl ester by careful base hydrolysis. (±)4(5)EpDPA is a CYP450 metabolite of DHA which can be further metabolized to the diol metabolite. There are no published reports on the biological activity of (±)4(5)-EpDPA methyl ester at this time.

Contezolid acefosamil (MRX-4), an orally active prodrug, is metabolized into Contezolid (MRX-I), an oxazolidinone derivative with potent in vitro efficacy against multidrug-resistant Gram-positive bacteria, including MRSA.

1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid initially identified in sheep vesicular gland microsome extracts containing COX and incubated with adrenic acid. It has also been detected in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid. This compound is believed to be produced by the elongation of AA to adrenic acid, followed by sequential metabolism by COX and PGE synthase.

C22 dihydro 1-Deoxyceramide (m18:0/22:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C22 dihydro 1-Deoxyceramide (m18:0/22:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found as the most prevalent dihydro deoxyceramide species in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

(±)19(20)-EpDTE is an oxylipin and an oxidative metabolite of docosapentaenoic acid (DPA), formed via cytochrome P450 (CYP) metabolism. It can be further metabolized to (±)19(20)-DiHDTE by epoxide hydrolase.

Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively. It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.

6-Hydroxymelatonin, a primary metabolite of Melatonin, is metabolized by CYP 1A2.

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO

Erythromycin glutamate is a macrolide bacteriostatic antibiotic. This antibiotic is metabolized through the liver and inhibits cytochrome enzyme P450A 3A41.

Methyl aminolevulinate is a prodrug that can be metabolized to Protoporphyrin IX. Methyl aminolevulinate is an agent used as a sensitizer in photodynamic therapy (PDT).

C6 L-erythro Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is metabolized by ceramide glucosyltransferase to form C6 L-erythro glucosylceramide. C6 L-erythro Ceramide is cytotoxic to U937 cells (IC50 = 18 μM).

8,11,14-Eicosatrienoic acid, also known as dihomo-γ-linolenic acid , is a polyunsaturated fatty acid (PUFA) produced from γ-linolenic acid by the action of fatty acid elongases. It can be metabolized by the cyclooxygenase pathway to produce 1-series prostaglandins (PGs) (e.g., PGE1). (±)14(15)-EpEDE is an EpEDE acid formed from 8,11,14-eicosatrienoic acid. This monoepoxide can be generated from the PUFA, in vitro, by the action of a strong oxidizing agent. Alternatively, this compound may be produced, in vivo, by epoxidation of the PUFA by cytochrome P450 epoxygenases. The biological properties of this compound are poorly understood.

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

Dehydro aripiprazole-d8 is a deuterated compound of Dehydro aripiprazole. Dehydro aripiprazole has a CAS number of 129722-25-4. Dehydroaripiprazole is the active metabolite of aripiprazole. Aripiprazole is an antipsychotic drug, which is metabolized by CYP3A4 and CYP2D6 and mainly forms dehydroaripiprazole. Dehydroaripiprazole has antipsychotic activity equivalent to aripiprazole.

Capecitabine-d11 is a deuterated compound of Capecitabine. Capecitabine has a CAS number of 154361-50-9. Capecitabine is a fluoropyrimidine carbamate belonging to the class of antineoplastic agents called antimetabolites. As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU); subsequently, 5-FU is metabolized to two active metabolites, 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) by both tumor cells and normal cells. FdUMP inhibits DNA synthesis and cell division by reducing normal thymidine production, while FUTP inhibits RNA and protein synthesis by competing with uridine triphosphate for incorporation into the RNA strand.