Drug Metabolite

Cat. No.

A29623

CAS No.

125481-61-0

BMY 28674

Synonyms: 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215

BMY 28674 (6-Hydroxybuspirone) is a significant drug metabolite of the anxiolytic agent buspirone, primarily metabolized by CYP3A4. This compound exhibits selective binding to the serotonin receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe, with effective concentrations (EC50s) of 4 μM and 1 μM, respectively. Additionally, BMY 28674 acts as an antagonist at dopamine D2, D3, and D4 receptors, demonstrating inhibitory constants (IC50s) of 3.1 μM, 4.9 μM, and 0.85 μM, respectively. Moreover, it inhibits the activity of organic cation transporters OCT1, OCT2, and OCT3 in human proximal tubule cells in a concentration-dependent manner, making it relevant for pharmacological studies involving these receptors and transporters.

Cat. No.

A61973

CAS No.

2238886-63-8

SCH-720881

SCH-720881 is the active metabolite of Rolapitant, a selective and long-acting neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. This compound exhibits significant anti-emetic properties, making it valuable for studies involving nausea and vomiting. SCH-720881 provides insights into the pharmacological effects of NK1 receptor modulation in various preclinical models, thereby facilitating research into anti-emetic therapies.

Cat. No.

A62847

CAS No.

947502-66-1

Prasugrel hydroxy thiolactone

Prasugrel hydroxy thiolactone is a key metabolite of Prasugrel, a potent and orally active antagonist of the P2Y12 receptor. This compound plays a significant role in inhibiting adenosine 5'-diphosphate (ADP)-induced platelet aggregation, making it valuable for investigating mechanisms of antiplatelet therapy and cardiovascular research. Its use is essential for understanding drug metabolism and efficacy in the context of thrombosis and cardiovascular disease management.

Cat. No.

A69942

CAS No.

253688-61-8

Desmethyl Bosentan

Synonyms: Ro 47-8634

Desmethyl Bosentan is an active metabolite of the endothelin receptor antagonist bosentan. It functions primarily by activating the pregnane X receptor (PXR), as demonstrated in CV-1 monkey kidney cells expressing the human receptor in a reporter assay at a concentration of 25 μM. This compound is valuable for studying drug metabolism and the regulatory pathways involved in pharmacokinetics and toxicology research.

Cat. No.

A70246

CAS No.

1251765-07-7

AR-C133913XX

AR-C133913XX is a metabolite of Ticagrelor, a reversible oral P2Y12 receptor antagonist. This compound is instrumental in studying platelet aggregation processes and the pharmacological effects of Ticagrelor in cardiovascular research. Its application extends to investigations of antiplatelet activity and therapeutic strategies for managing thrombotic disorders.

Cat. No.

A70274

CAS No.

142227-49-4

Carvedilol metabolite 4-Hydroxyphenyl Carvedilol

Synonyms: 4-Hydroxyphenyl Carvedilol; 4-Hydroxycarvedilol

4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol, functioning primarily as a drug metabolite. This compound plays a crucial role in pharmacokinetic studies, particularly in understanding the metabolism and efficacy of beta blockers and alpha-1 blockers. Its analysis is vital for examining drug interactions and assessing the therapeutic potential of cardiovascular agents.

Cat. No.

A70294

CAS No.

73851-70-4

Ranitidine S-oxide

Ranitidine S-oxide is a key metabolite of Ranitidine, a selective and orally active histamine H2-receptor antagonist. It exhibits a significant inhibitory effect on gastric secretion, with an IC50 of 3.3 μM. This compound is valuable for research applications focused on gastrointestinal physiology and the pharmacokinetics of H2-receptor antagonists.

Cat. No.

A70357

CAS No.

56392-16-6

a-Hydroxymetoprolol

a-Hydroxymetoprolol is a key metabolite of metoprolol, a beta-adrenergic blocker. This compound exhibits negligible adrenoreceptor blocking activity compared to its parent drug, making it an important molecule for understanding metoprolol's pharmacokinetics and metabolism. Research applications include studies on drug metabolism, therapeutic efficacy, and the effects of beta-blockade in cardiovascular contexts.

Cat. No.

A70390

CAS No.

210686-41-2

Hydroxyebastine

Hydroxyebastine is a metabolite of Ebastine, primarily targeting the histamine H1 receptor as an antagonist. This compound plays a significant role in understanding antihistamine metabolism and pharmacokinetics, as it is further converted to Carebastine by the cytochrome P450 enzymes CYP2J2 and CYP3A4. Hydroxyebastine is valuable for research into allergic response mechanisms and the efficacy of antihistaminic therapies.

Cat. No.

A70587

CAS No.

879292-24-7

Silodosin Glucuronide sodium

Synonyms: Silodosin β-D-glucuronide sodium

Silodosin Glucuronide sodium is the sodium salt of Silodosin β-D-glucuronide, a metabolite of the selective α1A-adrenergic receptor antagonist Silodosin. It exhibits high affinity for the α1A-AR, facilitating a Ki value of 0.036 nM. This compound is crucial for studying the pharmacokinetics and metabolic pathways of Silodosin, contributing to research applications in urology and cardiovascular studies.

Cat. No.

A70606

CAS No.

114869-83-9

Carvedilol Glucuronide

Carvedilol Glucuronide is a significant metabolite of the β/α-1 adrenergic receptor antagonist, Carvedilol. This compound demonstrates key biological activity by modulating β-adrenergic signaling and exhibits potential application in studying the metabolic pathway of Carvedilol. Research indicates that Carvedilol can inhibit lipid peroxidation and has properties as an antihypertensive agent, as well as an autophagy inducer that affects the NLRP3 inflammasome. Carvedilol Glucuronide serves as an important reagent for investigating drug metabolism and pharmacokinetics in cardiovascular research.

Cat. No.

A70632

CAS No.

47491-38-3

Desmethylazelastine

Desmethylazelastine is the primary active metabolite of Azelastine, functioning as a selective and high-affinity antagonist of the histamine H1 receptor. With a protein binding rate of 97% and an elimination half-life of 54 hours, it plays a significant role in the pharmacological effects of Azelastine. This compound is valuable for research applications involving allergic rhinitis, asthma, diabetic hyperlipidemia, and studies related to SARS-CoV-2.

Cat. No.

A70805

CAS No.

2293-21-2

Desmethyltrimipramine

Synonyms: DTRI

Desmethyltrimipramine is a metabolite of Trimipramine, serving as a 5-HT receptor antagonist. This compound exhibits notable antidepressant properties, contributing to its role in mood regulation. It is utilized in research to further understand the mechanisms of depression and the pharmacological effects of antidepressant therapies.

Cat. No.

A70849

CAS No.

910808-11-6

Netupitant metabolite Netupitant N-oxide

Synonyms: Netupitant N-oxide

Netupitant N-oxide is the primary metabolite of Netupitant, a highly selective antagonist of the neurokinin-1 (NK1) receptor. This compound is crucial for studying the pharmacokinetics and pharmacodynamics of Netupitant, contributing to the understanding of its efficacy and safety profile in clinical settings. It is particularly useful in research focusing on antiemetic therapies and the modulation of pain and anxiety pathways.

Cat. No.

A70887

CAS No.

34104-67-1

Reduced Haloperidol

Synonyms: Haloperidol metabolite II

Reduced Haloperidol, a primary metabolite of Haloperidol, functions as a dopamine receptor antagonist. It exhibits significant antipsychotic activity, primarily utilized in research related to schizophrenia and other psychotic disorders. This compound is instrumental in studies investigating the modulation of neurotransmitter systems, aiding in the reduction of hallucinations and delusions associated with these conditions.

Cat. No.

A70897

CAS No.

147663-04-5

7-Hydroxyrisperidone

Synonyms: 7-RispOH

7-Hydroxyrisperidone is a key metabolite of Risperidone, primarily known for its role as a serotonin 5-HT2 receptor antagonist and potent dopamine D2 receptor antagonist. This compound exhibits significant biological activity in modulating dopaminergic and serotonergic pathways, making it important for the study of psychiatric disorders. Its applications extend to pharmacokinetic research and the evaluation of drug metabolism, contributing valuable insights into the therapeutic effects and side effects associated with Risperidone treatment.

Cat. No.

A70960

CAS No.

3922-74-5

Diphenhydramine N-oxide

Diphenhydramine N-oxide is a metabolite of Diphenhydramine, a first-generation H1 receptor antagonist known for its anticholinergic properties. This reagent serves as an important tool for studying the pharmacokinetics and metabolic pathways of Diphenhydramine, particularly in relation to its central nervous system effects. Researchers can utilize Diphenhydramine N-oxide to investigate its role in drug metabolism and potential therapeutic implications in various biological systems.

Cat. No.

A70991

CAS No.

909800-36-8

THRX-195518

THRX-195518 is the primary metabolite of Revefenacin, a selective and long-acting muscarinic antagonist primarily targeting the lungs. This compound is relevant for research focused on chronic obstructive pulmonary disease (COPD), facilitating investigations into pulmonary pharmacology and the therapeutic potential of muscarinic modulation in respiratory disorders.

Cat. No.

A73583

CAS No.

57898-80-3

N-Desbutyroyl acebutolol

Synonyms: Deacyl acebutolol; M and B 17127

N-Desbutyroyl acebutolol is a metabolite of the beta-blocker acebutolol. This compound is primarily studied for its relevance in pharmacokinetics and metabolism research. It serves as a useful tool for investigating the biotransformation pathways of acebutolol and assessing the pharmacological implications of its metabolites in cardiovascular studies.