metabolites

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

Norgestimate is an acetylated progestinused in combination with ethinyl estradiol as an oral contraceptive.

Ipriflavone metabolites (IV) are the metabolic byproducts of Ipriflavone.

LSN2839567 (Abemaciclib metabolite M2) is the active metabolite of Abemaciclib, a potent CDK4 and CDK6 inhibitor (IC50s: 1-3 nM) with anticancer activity.LSN2839567 inhibits CDK9.LSN2839567 inhibits cell growth and cell cycle progression in a concentration-dependent manner. cell growth and cell cycle progression in a concentration-dependent manner and can be used to study breast and lung cancer.

20-HETE belongs to endogenous metabolites (natural products) and is a protein kinase C (PKC) pathway activator that promotes ACSL4 ubiquitination and degradation through upregulation of FBXO10, possessing regulatory properties on cell proliferation and migration. This compound is used in research related to prostate tumors and cardiac hypertrophy.

p-Cresyl Sulfate is the major uremic toxin present in the blood of patients with chronic kidney disease and is derived from the metabolites of tyrosine and phenylalanine in the liver.

6PPD-Q (6PPD-Quinone) is an environmental pollutant that can target CNR2, CNR1, AA2AR, LCAT and TRPA1. Among them, CNR2 has the highest binding affinity and may act as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q can damage the sperm quality and induce the impairment of male reproductive ability in mice. 6PPD-Q can induce intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolytic metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

5,6-Dihydro-5-methyluracil (Dihydrothymine) is an intermediate breakdown product of thymine.

Fomepizole (4-Methylpyrazole) is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole(4-Methylpyrazole) is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.

Erdosteine (RV 144) is a homocysteine-derived thiol derivative with mucolytic and free radical scavenging properties. Erdosteine and its metabolites modulate mucus production and viscosity, by which facilitating mucociliary transport and improving expectoration. This agent also suppresses the chemical-induced cough reflex as well as protects lung tissues from damages caused by cigarette smoking mediated through free radicals scavenging.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

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.

Sodium 2-mercaptoethanesulfonate (Uromitexan) is a sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from antineoplastic agents, such as ifosfamide or cyclophosphamide.

Bromhexine Impurity B reagent used in the preparation of Ambroxol and Bromhexine (B678600) metabolites Ambroxol EP Impurity E.

Thioacetamide (TAA) is an indirect hepatotoxin commonly used to induce experimental liver injury. It is metabolized by CYP2E1 into reactive metabolites that covalently bind to proteins and lipids, leading to oxidative stress and centrilobular necrosis, hepatocyte death, and M1/M2 macrophage-dominated inflammation. TAA is widely used to establish models of chronic liver fibrosis, hepatic encephalopathy, and liver cancer.

Pyridoxal phosphate (Vitamin B6 phosphate) is the active form of vitamin B6 and a coenzyme for many pyridoxal phosphate (PLP)-dependent enzymes. PLP is involved in numerous enzymatic transamination, decarboxylation and deamination reactions; it is necessary for the synthesis of amino acids and amino acid metabolites, and for the synthesis and/or catabolism of certain neurotransmitters, including the conversion of glutamate into gamma-aminobutyric acid (GABA) and levodopa into dopamine. PLP can be used as a dietary supplement in cases of vitamin B6 deficiency. Reduced levels of PLP in the brain can cause neurological dysfunction.

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

(S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a tart-tasting organic dicarboxylic acid found in many sour foods, such as apples, and contributes to the sourness of green apples and tartness of wine, although its concentration decreases with fruit ripeness (wikipedia). In its ionized form, it is called malate, an intermediate in the TCA cycle alongside fumarate, and can be formed from pyruvate through anaplerotic reactions. In humans, malic acid is derived from food sources and synthesized in the body via the citric acid cycle in mitochondria, playing a crucial role in energy production under both aerobic and anaerobic conditions. Under aerobic conditions, malate is oxidized to oxaloacetate, providing reducing equivalents via the malate-aspartate redox shuttle, while during anaerobic conditions, its simultaneous reduction to succinate and oxidation to oxaloacetate removes excess reducing equivalents, reversing hypoxia's inhibition of glycolysis and energy production. Studies on rats have shown that tissue malate depletes following exhaustive physical activity, suggesting that malic acid deficiency may cause physical exhaustion. Administering malic acid to rats has been shown to elevate mitochondrial malate, increasing mitochondrial respiration and energy production.

Produced in the gut microflora as one of the three main metabolites formed from the catechin diet. Its use in the production of glycol benzoates for the application of plasticizer in adhesive formulations is increasing. It is also used in the manufacture

O-PHOSPHO-L-SERINE is an ester of serine and phosphate, which are normal metabolites in human biofluids.O-phospho-L-serine is a phagocytosis inhibitor that inhibits glial cell proliferation and cone cell regeneration after photodamage.

Nicotinuric acid is an acyl glycine which is normally minor metabolites of fatty acids. Acyl glycines are produced through the action of glycine N-acyltransferase.

N-Methylnicotinamide is one of the endogenous metabolites that ameliorates endothelial dysfunction.

All-trans-retinal (Vitamin A aldehyde) is a one of the major vitamin A metabolites in the retina. All-trans-RAL is regenerated to the visual chromophore, 11-cis-retinal in physiological conditions.