Catalog No.
Product Name
Application
Product Information
Citations
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CYP1A1 Inducer
Methysticin is a kavalactone derived from kava extract, primarily acting as an inducer of CYP1A1. This compound is relevant in studies investigating metabolic enzyme modulation and its impact on drug metabolism. Additionally, it has potential implications in understanding the biochemical pathways associated with liver function and detoxification processes. -
CYP17A1 Lyase Inhibitor
BMS-351 is a potent, orally active nonsteroidal inhibitor of CYP17A1 lyase, demonstrating IC50 values of 19 nM for human CYP17A1 and 4 nM for cynomolgus monkey CYP17A1. This compound is primarily utilized in research focused on castration-resistant prostate cancer, providing insights into hormonal regulation and potential therapeutic interventions in this challenging malignancy. -
CYP1B1 Inhibitor
(E/Z)-DMU2105 is a selective inhibitor of CYP1B1, demonstrating potent inhibition with an IC50 value of 10 nM in yeast-derived microsomes and 63.65 nM in live recombinant yeast and human HEK293 kidney cells. This compound is valuable for research focused on cancer, glaucoma, ischemia, and obesity, offering insights into the role of CYP1B1 in various biological processes. Its specificity and potency make it a suitable tool for elucidating the function of this key enzyme in disease contexts. -
CYP11B2 Inhibitor
CYP11B2-IN-2 is a potent inhibitor of the aldosterone synthase enzyme CYP11B2, exhibiting an IC50 value of 0.3 nM. This compound is labeled with 18F, enabling its application as a positron emission tomography (PET) tracer for the diagnosis of primary aldosteronism. Its high specificity and efficacy make it a valuable tool for research in endocrine disorders and adrenal function. -
CYP2C9/VKOR Inhibitor
10-Hydroxywarfarin is a potent inhibitor of CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR), exhibiting IC50 values of 1.6 µM and 80 ng/mL, respectively. This compound serves as a valuable tool in pharmacological research, particularly in studies related to anticoagulation therapies and vitamin K metabolism. Its role in influencing coagulation pathways makes it relevant for investigations into therapeutic strategies for thrombosis and related disorders. -
CYP1B1 Inhibitor
(E/Z)-DMU2139 is a potent and selective inhibitor of CYP1B1, exhibiting an IC50 value of 4 nM. This compound serves as a valuable tool for investigating the role of CYP1B1 in various biological processes and disease models. Its specificity and efficacy make it suitable for research aimed at understanding the mechanisms underlying CYP1B1-related pathways and the development of targeted therapies. -
HMG-CoA Reductase (HMGCR) Inhibitor
SKF 104976 is a selective inhibitor of HMG-CoA reductase (HMGCR), demonstrating significant inhibitory activity in biochemical assays. It effectively reduces cholesterol synthesis in Hep G2 cells by inhibiting the incorporation of [14C]acetate at concentrations as low as 2 nM, leading to the accumulation of lanosterol and a substantial decrease in HMGR activity by 40-70%. Importantly, SKF 104976 does not influence low-density lipoprotein uptake or degradation, indicating a distinct regulatory mechanism for HMGR and low-density lipoprotein receptors. This compound serves as a valuable tool for studying cholesterol metabolism and the regulation of sterol synthesis pathways in cellular models. -
CYP2C9 Inhibitor
Cloperidone is an inhibitor of cytochrome P450 2C9 (CYP2C9), demonstrating an IC50 of 17.7 μM. This compound has shown cytotoxic effects in HepG2 cells expressing CYP2C9, with a survival rate of 60% at a concentration of 10 μM. Cloperidone is valuable for studies investigating CYP2C9-related metabolic pathways and the effects of its inhibition in cellular models. -
Drug Metabolites
7α-Hydroxy-DHEA (7α-Hydroxydehydroepiandrosterone) is a 7α-hydroxylated metabolite of dehydroepiandrosterone (DHEA), generated through the action of intracellular steroid 7α-hydroxylases, notably P450 2A1. This compound exhibits biological activity akin to DHEA while lacking the potential for androgenic or estrogenic conversion. 7α-Hydroxy-DHEA enhances the activity of thermogenic enzymes, including mitochondrial sn-glycerol-3-phosphate dehydrogenase and cytosolic malic enzyme, promoting heat production and decreasing food utilization efficiency. This metabolite presents a promising avenue for research in obesity, metabolic diseases, and adrenal carcinoma. -
CYP2B4/CYP2E1 Inhibitor
4-Phenyl-1,2,3-thiadiazole is an inhibitor of cytochrome P450 enzymes CYP2B4 and CYP2E1. This compound effectively obstructs the oxidation of 1-phenylethanol to acetophenone, making it valuable for studies related to drug metabolism and enzymatic activity. Its ability to selectively inhibit these enzymes positions it as a significant tool for research in pharmacology and toxicology. -
CYP4Z1 Inhibitor
CYP4Z1-IN-2 is a reversible inhibitor of the enzyme CYP4Z1, displaying a Ki value of 2.2 μM. This compound effectively reduces the production of 14,15-EET in breast cancer cells and demonstrates an IC50 of 5.9 μM in inhibiting the CYP4Z1-mediated Luc-BE O-debenzylation reaction. CYP4Z1-IN-2 serves as a valuable tool for research focused on the role of CYP4Z1 in cancer biology and associated signaling pathways. -
Drug Metabolite
Paraxanthine, a primary metabolite of caffeine, exerts neuroprotective effects by stimulating Ryanodine Receptor Channels, thereby offering protection against dopaminergic cell death. This compound is valuable in research focusing on neurodegenerative diseases and the role of caffeine metabolites in cellular signaling and survival pathways. Its utility extends to studies investigating the therapeutic potential of caffeine-related compounds in brain health. -
Endogenous Metabolite
N-Methylnicotinamide is an endogenous metabolite primarily involved in thrombotic regulation through its antithrombotic properties. It functions by promoting the production and release of prostacyclin, which inhibits the development of arterial thrombosis. This compound is synthesized via the N-methylation of nicotinamide, catalyzed by N-methyltransferase, and plays a crucial role in the nicotinate and nicotinamide metabolic pathways, making it relevant for research in cardiovascular health and metabolic processes. -
Drug Metabolite
3,4-Dihydroxybenzeneacetic acid is a key metabolite of dopamine, primarily associated with neuronal activity. This compound plays a significant role in the metabolism of neurotransmitters and can be used in research studies focused on neurochemistry and dopamine-related disorders. Its analysis aids in understanding the biochemical pathways involved in neurotransmission and the effects of dopamine in various neurological conditions. -
Drug Metabolite
4'-Hydroxy diclofenac is a drug metabolite derived from diclofenac, primarily processed by cytochrome P450 2C9 (CYP2C9). This compound exhibits anti-inflammatory and analgesic activities, making it valuable in pharmacological research focused on pain management and inflammation. Its role as a bioactive metabolite offers insights into drug metabolism and therapeutic efficacy. -
Drug Metabolite
Ternidazole hydrochloride is a hydroxymetabolite of nitroimidazole that targets protozoa, exhibiting notable antiprotozoic activity. It is primarily utilized in research related to drug metabolism and the pharmacokinetics of nitroimidazole derivatives. Its applications extend to studies of parasitic infections and the evaluation of therapeutic efficacy against protozoal pathogens. -
Drug Metabolite
1-Methylxanthine is a key metabolite derived from caffeine and theophylline, primarily functioning as a drug metabolite. It has been shown to enhance the radiosensitivity of tumor cells, making it relevant for cancer research and therapeutic studies involving radiation treatment. Its role in understanding drug metabolism and potential impacts on treatment efficacy make it an important reagent in pharmacological and biochemical investigations. -
Drug Metabolite
N-Desmethyl imatinib is an active metabolite of Imatinib, primarily targeting the c-Abl kinase by binding to its catalytic domain, thus inhibiting substrate phosphorylation. This compound exhibits significant biological activity by inhibiting c-Abl-mediated α-synuclein activation and modulating downstream inflammatory signaling pathways, which leads to apoptosis in K562 human leukemia cells. Research applications include the investigation of pediatric gastrointestinal stromal tumors, chronic myeloid leukemia, and potential implications in neurodegenerative disorders such as Parkinson's disease. Elevated plasma levels of N-Desmethyl imatinib following certain viral infections can offer insights into its therapeutic roles. -
Drug Metabolite
1-Methyluric acid is a metabolite of various drugs that primarily targets the urinary bladder mucosa. It is associated with increased levels of blood glucose, insulin, triglycerides, and cholesterol. This compound is relevant in research pertaining to metabolic disorders and the pharmacokinetics of drug metabolism, providing insights into the biochemical pathways involved in energy regulation and lipid metabolism. -
Endogenous Metabolite
4-Hydroxyestradiol is an endogenous metabolite of estradiol that acts as a potent estrogen receptor antagonist. This compound exhibits carcinogenic properties and demonstrates mutagenic activity in breast epithelial cells, indicating its role in cellular transformation processes. Its competitive inhibition of estradiol binding to the estrogen receptor, with a Ki value of 0.48 nM, makes it a valuable tool for studying estrogen-related pathways and breast cancer biology. -
Drug Metabolite
Lignocaine N-oxide is a metabolite of lidocaine, primarily formed through the metabolism of lidocaine in liver microsomes. This compound serves as an important biomarker in pharmacokinetic studies, aiding in the understanding of lidocaine's metabolic pathways. It is utilized in research to investigate drug metabolism and potential pharmacological effects associated with lidocaine administration. -
Drug Metabolite
N-Deschlorobenzoyl indomethacin is a primary metabolite of indomethacin that lacks the N-p-chlorobenzoyl group. This alteration results in a significant reduction of its inhibitory activity against the enzymes AKR1C2 and AKR1C3, with an IC50 of 100 μM for AKR1C2 and an IC50 greater than 100 μM for AKR1C3, indicating no selectivity. This compound serves as a useful tool for studying the metabolic pathways and pharmacokinetics of indomethacin in various research applications. -
Drug Metabolite
N-Desmethyl Clomipramine Hydrochloride is a primary plasma N-desmethyl metabolite of Clomipramine, a tricyclic antidepressant. This compound serves as a significant biomarker in pharmacokinetic studies and therapeutic monitoring of Clomipramine treatment. Its relevance in understanding drug metabolism and efficacy makes it a valuable reagent in clinical and pharmaceutical research applications. -
Drug Metabolite
DL-Laudanosine, a metabolite of Atracurium and Cisatracurium, acts on the central nervous system by crossing the blood-brain barrier. It is known to induce excitatory responses and has been linked to seizure activity. This compound is used in research related to neuromuscular blockade and CNS effects of anesthetic agents. -
Drug Metabolite
3'-Hydroxy Repaglinide is a primary metabolite of Repaglinide, primarily formed through CYP2C8 enzymatic activity. As a carbamoylmethyl benzoic acid (CMBA) derivative, it plays a significant role in the pharmacokinetics of Repaglinide, a drug used for the management of type II diabetes. This compound is essential for understanding the metabolism and efficacy of Repaglinide in clinical research and drug development. -
Drug Metabolite
Clopidogrel carboxylic acid hydrochloride is an inactive metabolite of the antiplatelet agent clopidogrel, serving as a reference standard for the analysis of clopidogrel metabolism. It constitutes approximately 85% of the circulating clopidogrel, formed by hydrolysis of the active compound via esterase activity. This metabolite is essential for evaluating the pharmacokinetics and bioavailability of clopidogrel in both clinical and research environments, facilitating a deeper understanding of its therapeutic profile. -
Drug Metabolite
4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole, produced via hepatic oxidative metabolism. This compound exhibits a plasma concentration that correlates with the administered dosage of Fomepizole and has a relatively short half-life. It acts as an inhibitor of alcohol dehydrogenase (ADH) in humans and monkeys; however, its inhibition constant is significantly higher than that of its parent compound, suggesting a minimal in vivo impact. It is primarily used for research on metabolic pathways and drug interactions. -
Endogenous Metabolite
Diclofenac acyl glucuronide (D-1-O-G) is an endogenous metabolite that results from the conjugation of diclofenac. This compound plays a significant role in the pharmacokinetics of non-steroidal anti-inflammatory drugs (NSAIDs) and is implicated in gastrointestinal toxicity, particularly small intestinal ulceration in rat models. It serves as a valuable tool for studying drug metabolism and the effects of NSAIDs on the digestive system in research applications. -
Drug Metabolite
Eicosapentaenoic acid methyl ester is a metabolite of monogalactosyl diacylglycerol, known for its role in inducing apoptosis. This compound demonstrates key biological activities that could be beneficial in cancer research, specifically in studies focused on apoptosis pathways and therapeutic interventions. Its applications extend to investigating the metabolic pathways of drug degradation and the evaluation of anticancer effects in various biological settings. -
Drug Metabolite
Apovincaminic acid hydrochloride salt is an active metabolite of Vinpocetine, primarily targeting neuroprotection. It possesses the ability to penetrate the blood-brain barrier, making it suitable for research into neuronal health and cognitive enhancement. This compound is utilized in studies focusing on neuroprotection and potential therapeutic applications in neurodegenerative disorders. -
Drug Metabolite
7-Hydroxymethotrexate is a key metabolite of Methotrexate, primarily produced through the hepatic metabolism of the drug. It is involved in the inhibition of dihydrofolate reductase, thereby blocking the conversion of folic acid to tetrahydrofolate and subsequently disrupting DNA synthesis. This compound is significant in pharmacokinetic studies and therapeutic monitoring of Methotrexate, aiding in understanding its efficacy and safety profiles in various treatment regimens. -
Drug Metabolite
Niraparib metabolite M1 is a bioactive metabolite of the poly(ADP-ribose) polymerase (PARP) inhibitor niraparib. This compound retains the biological effects associated with PARP inhibition, contributing to the understanding of niraparib's pharmacokinetics and pharmacodynamics. Niraparib metabolite M1 is relevant for investigating the mechanisms of action and therapeutic effects of PARP inhibitors in cancer research, particularly in the context of DNA repair and cellular response to genotoxic stress. -
Drug Metabolite
Monobenzyl phthalate is an aromatic alkyl chain monophthalate and a known drug metabolite. It exhibits significant antiandrogenic properties and has been shown to inhibit male reproductive development in rat fetuses. This compound is valuable for research focused on endocrine disruption and developmental toxicity assessments in toxicology studies. -
Drug Metabolite
Tofacitinib metabolite-1 is a metabolite derived from Tofacitinib, a selective inhibitor of Janus kinase (JAK) enzymes. This compound plays a critical role in pharmacokinetic and metabolic studies of Tofacitinib, facilitating the understanding of its bioavailability, metabolism, and overall therapeutic efficacy. Researchers can utilize Tofacitinib metabolite-1 to investigate its biological activity and potential impacts on various signaling pathways involved in inflammatory processes. -
Drug Metabolite
Quetiapine sulfoxide dihydrochloride is a primary metabolite of the second-generation antipsychotic quetiapine. This compound functions as a 5-HT receptor agonist and a dopamine receptor antagonist, contributing to its pharmacological effects. It is commonly utilized in research related to neuropharmacology and metabolic profiling of antipsychotic drugs, offering insights into the drug's therapeutic activity and safety profile. -
Drug Metabolite
Ribavirin carboxylic acid is a key metabolite of Ribavirin, primarily involved in antiviral mechanisms. This compound exhibits biological activity through its interaction with viral RNA polymerases, contributing to the inhibition of viral replication. It is commonly used in research to study the pharmacokinetics and therapeutic effects of Ribavirin, as well as to explore antiviral strategies against related viral infections. -
Drug Metabolite
Olanzapine N-oxide is a drug metabolite derived from the antipsychotic medication olanzapine. This compound is primarily studied for its role in the metabolic pathways of antipsychotics, specifically involving N-oxidation and N-demethylation processes, which are mediated by distinct enzymatic activities. Research indicates that the plasma concentration and clearance of Olanzapine N-oxide are influenced by multiple factors rather than being determined by single variables such as genotype or smoking status. -
Drug Metabolite
Ternidazole is a hydroxymetabolite of nitroimidazole, acting primarily as a drug metabolite. It exhibits notable antiprotozoal activity, making it relevant in the study of protozoan infections. This compound is utilized in research to investigate drug metabolism and the therapeutic efficacy of nitroimidazole derivatives. -
Drug Metabolite
Imipramine N-oxide is a primary metabolite of the tricyclic antidepressant Imipramine, classified as a tertiary amine. This compound exhibits neuropharmacological activity and is critical for studies on antidepressant metabolism and pharmacokinetics. Research applications include investigations into drug efficacy, side effects, and the metabolic pathways of tricyclic antidepressants in both in vitro and in vivo models. -
Levofloxacin Minor Metabolite
Levofloxacin N-oxide is a minor metabolite of the fluoroquinolone antibiotic Levofloxacin, primarily functioning as an antibacterial agent targeting DNA gyrase and topoisomerase IV. It demonstrates minimal genotoxic risks, which may provide insights into the safety profile of Levofloxacin. This compound is valuable for research applications focused on antibiotic metabolism and the mechanistic studies of bacterial resistance. -
Drug Metabolite
1,3-Dimethyluric acid is a metabolite of theophylline, primarily involved in purine metabolism. This compound is significant in understanding metabolic pathways and can serve as a biomarker in studies related to theophylline pharmacokinetics. Additionally, it can contribute to research on urinary calculi formation due to its role as a purine component. -
Metabolin
5-Hydroxyomeprazole is the primary metabolite of Omeprazole, functioning as a proton pump inhibitor. It inhibits gastric acid secretion by targeting the proton pump in gastric parietal cells, thereby reducing acidity. This compound is valuable in research related to gastrointestinal physiology and pharmacokinetics, as well as in studies examining the effects of acid suppression on various physiological processes. -
Drug Metabolite
15-Acetyl-deoxynivalenol is a toxic trichothecene metabolite of deoxynivalenol, primarily affecting cellular health. This compound demonstrates significant toxicity in HepG2 liver cells, making it a valuable tool for studying the toxicological impacts of mycotoxins in food safety research. Its role in cellular responses to xenobiotic exposure offers insights into metabolic pathways and potential health risks associated with cereal contaminants. -
Drug Metabolite
2-Aminoflubendazole is a prominent metabolite of Benzimidazoles, a class of compounds known for their efficacy against fungi, protozoa, and helminths. This compound serves as a valuable tool in research applications aimed at understanding the metabolic pathways and pharmacological effects of benzothiazole derivatives. Its role in studying drug metabolism and toxicology offers important insights into the therapeutic potential and safety profiles of related therapeutic agents. -
Drug Metabolite
Ingenol disoxate is a drug metabolite known for its potential to mitigate actinic keratosis. It functions through a mechanism that may enhance cellular proliferation and modulate immune responses. This compound is valuable for research focused on dermatological conditions and the development of topical treatments for skin disorders. -
Drug Metabolite
Biprofen is a nonsteroidal anti-inflammatory drug metabolite that primarily targets cyclooxygenase enzymes. It exhibits significant anti-inflammatory and analgesic properties, making it valuable in research related to pain management and inflammatory diseases. Biprofen is utilized in studies investigating drug metabolism and the effects of anti-inflammatory therapies. -
Drug Metabolite
3-Hydroxy Medetomidine is a primary metabolite of the α2-adrenergic receptor agonist medetomidine. This compound exhibits important biological activity as it participates in modulating adrenergic signaling pathways. Research applications include studies on drug metabolism and the pharmacokinetics of sedatives in both veterinary and medical contexts. -
Drug Metabolite
T-705RMP ammonium is the ammonium derivative of T-705RMP and serves as a drug metabolite. It exhibits weak inhibition of inosine monophosphate dehydrogenase (IMPDH), which plays a critical role in purine biosynthesis. This compound is useful for investigating metabolic pathways and evaluating the pharmacokinetics of T-705RMP in biological research settings. -
Drug Metabolite
Hydroxyhexamide is a pharmacologically active metabolite of Acetohexamide that primarily functions as a hypoglycemic agent. This compound plays a significant role in glucose metabolism and insulin regulation, making it relevant in the study of diabetes and other metabolic disorders. Its biological activity is of particular interest for research applications focused on the development of antidiabetic therapies and understanding the pharmacokinetics of related compounds. -
Drug Metabolite
Dopamine 4-sulfate is an inactive metabolite of the neurotransmitter dopamine, generated through the catalytic action of the sulfotransferase enzyme SULT1A3. Although it exists in lower concentrations compared to other sulfated forms such as dopamine 3-O-sulfate, its presence in the brain and circulation is relevant for studies on dopamine metabolism and regulation. This compound is utilized in biochemical research examining dopamine's pharmacokinetics and its role in neurological pathways.
