Drug Metabolite

Cat. No.

A69920

CAS No.

67739-71-3

3-Hydroxyflunitrazepam

Synonyms: 3-OH FNTZ

3-Hydroxyflunitrazepam is the principal metabolite of Flunitrazepam, formed through 3-hydroxylation by the enzyme CYP3A4. This metabolite constitutes over 80% of Flunitrazepam's metabolic pathway in liver microsomes, highlighting its relevance in pharmacokinetics. The formation of 3-Hydroxyflunitrazepam is significantly inhibited by CYP3A4 inhibitors such as Ketoconazole and Ritonavir, suggesting crucial implications for drug-drug interactions in therapeutic applications and metabolic studies.

Cat. No.

A70103

CAS No.

133525-01-6

Zidovudine O-β-D-glucuronide sodium

Synonyms: 3'-Azido-3'-deoxythymidine β-D-glucuronide sodium

Zidovudine O-β-D-glucuronide sodium is the principal metabolite of Zidovudine, a nucleoside reverse transcriptase inhibitor (NRTI) utilized in HIV treatment. This compound serves as a versatile click chemistry reagent, featuring an azide group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. Additionally, it is capable of undergoing strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN groups, making it valuable for various molecular applications in chemical biology and pharmacokinetics research.

Cat. No.

A70113

CAS No.

47132-16-1

(E)-10-Hydroxynortriptyline

Synonyms: E-10-OH-NT

(E)-10-Hydroxynortriptyline is a metabolite of the tricyclic antidepressant Nortriptyline, primarily targeting norepinephrine reuptake. This compound exhibits approximately 50% of the potency of Nortriptyline as an inhibitor of neuronal norepinephrine uptake in vitro, while demonstrating reduced anticholinergic effects. E-10-OH-NT serves as a valuable tool for studying the pharmacological profile of tricyclic antidepressants and their metabolites in depression and related disorders.

Cat. No.

A70123

CAS No.

23981-47-7

α-Demethylnaproxen

α-Demethylnaproxen is the principal metabolite of Nabumetone, an orally active selective cyclooxygenase-2 (COX-2) inhibitor known for its anti-inflammatory properties. This compound plays a significant role in understanding the pharmacokinetics and biological effects of Nabumetone. Research applications include studies on inflammation, pain modulation, and the evaluation of COX-2 inhibition in various biological systems.

Cat. No.

A70125

CAS No.

834919-19-6

Edoxaban M4

Synonyms: D21-2393

Edoxaban M4 is the active metabolite of Edoxaban, a selective and potent inhibitor of factor Xa (FXa). This compound exhibits concentration-dependent matrix effects and serves as a critical tool for evaluating anticoagulation therapies. It is primarily utilized in pharmacological research to study the mechanisms of thrombin generation and its implications in coagulation disorders.

Cat. No.

A70126

CAS No.

16110-10-4

Acetaminophen glucuronide

Synonyms: APAP-glu

Acetaminophen glucuronide is a key inactive metabolite of Acetaminophen, primarily formed through glucuronidation. This compound serves as an important biomarker in pharmacokinetic studies, aiding in the assessment of Acetaminophen metabolism and its potential effects on liver function. Research applications include investigations into drug interactions and the metabolic pathways of COX-2 inhibitors.

Cat. No.

A70143

CAS No.

25222-43-9

4-Hydroxymethylpyrazole

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.

Cat. No.

A70149

CAS No.

18913-84-3

Nordeprenyl

Synonyms: Desmethylselegiline

Nordeprenyl is a metabolite of Deprenyl, functioning primarily as a selective and irreversible inhibitor of MAO-B. This compound also serves as a versatile click chemistry reagent, possessing an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing substrates. Nordeprenyl's unique properties make it valuable for research applications involving metabolic studies and the development of bioconjugates in chemical biology.

Cat. No.

A70153

CAS No.

1476777-06-6

Niraparib metabolite M1

Synonyms: Niraparib carboxylic acid metabolite M1; M1 metabolite of niraparib

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.

Cat. No.

A70162

CAS No.

503610-43-3

Rosuvastatin lactone

Rosuvastatin lactone is a metabolite of Rosuvastatin, functioning as an inhibitor of HMG-CoA reductase. This compound is integral for studies related to lipid metabolism and cholesterol synthesis regulation. Its biological activity is essential for exploring the pharmacological effects and therapeutic mechanisms associated with statin medications.

Cat. No.

A70163

CAS No.

1640971-51-2

Tofacitinib metabolite-1

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.

Cat. No.

A70179

CAS No.

134521-16-7

CGP 44 645

CGP 44 645 is a methanol metabolite of Letrozole, serving as a molecular marker for assessing the metabolic kinetics of Letrozole in vitro using microsomes. This compound can provide insights into the metabolic profile, particularly highlighting potential sex-specific variations in its levels within rat liver microsomes. Research applications include pharmacokinetic studies and investigations into the metabolism of aromatase inhibitors.

Cat. No.

A70197

CAS No.

503612-76-8

O-Desmethyl apixaban

O-Desmethyl apixaban is a metabolite of the anticoagulant apixaban, which functions as a highly selective and reversible inhibitor of Factor Xa, exhibiting a Ki of 0.08 nM in humans and 0.17 nM in rabbits. This compound is essential for studying the pharmacokinetics and pharmacodynamics of apixaban, contributing to research on its anticoagulant activity and safety profiles. Its role in drug metabolism further aids investigations into potential drug interactions and therapeutic outcomes in various cardiovascular conditions.

Cat. No.

A70202

CAS No.

92340-57-3

5-Hydroxyomeprazole

Synonyms: Hydroxyomeprazole

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.

Cat. No.

A70209

CAS No.

1300690-48-5

AP24600

AP24600 is an inactive metabolite of Ponatinib, a potent inhibitor of BCR-ABL tyrosine kinase. This compound serves as a valuable tool for understanding the pharmacokinetics and metabolic pathways of Ponatinib in cellular models. Its characterization can aid in the exploration of drug metabolism and efficacy in various research applications, particularly in the context of targeted cancer therapies.

Cat. No.

A70241

CAS No.

133627-24-4

12-Hydroxynevirapine

Synonyms: 12-hydroxy-NVP; 12-OH-NVP

12-Hydroxynevirapine is an oxidative metabolite of Nevirapine, a non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV-1 infections. This compound is noteworthy for its role in potentially contributing to hepatotoxicity and skin rashes associated with Nevirapine. In biological systems, 12-Hydroxynevirapine may be bioactivated by sulphotransferases (SULTs), leading to the formation of the reactive metabolite 12-Sulphoxy-nevirapine. Its analysis is essential for understanding the pharmacokinetics and safety profile of Nevirapine.

Cat. No.

A70257

CAS No.

2130882-23-2

PTX-M

PTX-M is an oxidized metabolite of Pentoxifylline, a known phosphodiesterase inhibitor. This compound is primarily utilized in the investigation of peripheral vascular, inflammatory, and immune diseases. PTX-M's role as a metabolite allows for specific studies into metabolic pathways and can help elucidate the pharmacodynamic effects associated with Pentoxifylline treatment.

Cat. No.

A70263

CAS No.

1221722-10-6

Sonidegib metabolite M48

Sonidegib metabolite M48 is the primary circulating metabolite of the hedgehog pathway inhibitor Sonidegib. M48 exhibits a significantly prolonged Tmax of 60 hours, suggesting a distinct pharmacokinetic profile compared to its parent compound. This metabolite is essential for the investigation of Sonidegib's therapeutic effects and pharmacodynamics in cancer research, particularly in the context of tumors driven by aberrant hedgehog signaling.

Cat. No.

A70288

CAS No.

417717-04-5

O-Demethyl Lenvatinib

O-Demethyl Lenvatinib is a significant metabolite of Lenvatinib, a multi-targeted oral tyrosine kinase inhibitor. It primarily targets vascular endothelial growth factor receptors (VEGFR1-3), fibroblast growth factor receptors (FGFR1-4), platelet-derived growth factor receptor (PDGFR), KIT, and RET, demonstrating potent antitumor activity. This reagent is valuable for research applications that explore the biological effects and pharmacokinetics of Lenvatinib in various cancer models.

Cat. No.

A70293

CAS No.

319491-68-4

N-Desalkyludenafil

N-Desalkyludenafil is a primary metabolite of Udenafil, a selective phosphodiesterase type 5 (PDE5) inhibitor. This compound is important for investigating the pharmacokinetics and metabolism of Udenafil in the context of erectile dysfunction research. Its characterization aids in understanding therapeutic effects and potential side effects related to PDE5 inhibition.

Cat. No.

A70299

CAS No.

910297-52-8

Dasatinib N-oxide

Dasatinib N-oxide is a minor metabolite of Dasatinib, which functions primarily as a potent and orally bioavailable dual inhibitor of Src and Bcr-Abl kinases. This compound plays a significant role in the pharmacokinetics and metabolism of Dasatinib, contributing to understanding its therapeutic effects and potential side effects. Researchers can utilize Dasatinib N-oxide to study its biological activity and implications in cancer treatment, particularly in relation to chronic myeloid leukemia and other Src-related malignancies.

Cat. No.

A70301

CAS No.

110374-16-8

4-Desmethoxy Omeprazole

4-Desmethoxy Omeprazole is an active metabolite of the proton pump inhibitor Omeprazole, primarily targeting acid-related gastrointestinal disorders. This compound exhibits competitive inhibition of CYP2C19, with a Ki value ranging from 2 to 6 μM, influencing drug metabolism. Additionally, 4-Desmethoxy Omeprazole demonstrates antimicrobial activity by inhibiting the growth of both Gram-positive and Gram-negative bacteria, making it relevant for various pharmacological and microbiological research applications.

Cat. No.

A70313

CAS No.

126313-98-2

(Rac)-3′-Hydroxy simvastatin

(Rac)-3′-Hydroxy simvastatin is a drug metabolite derived from Simvastatin, which acts as a competitive inhibitor of HMG-CoA reductase. With a Ki value of 0.2 nM, it plays a crucial role in cholesterol biosynthesis regulation. This compound is relevant in pharmacokinetic studies and investigations into the metabolic pathways of statins.

Cat. No.

A70334

CAS No.

176655-56-4

Hydroxy ritonavir

Hydroxy ritonavir is a metabolite of the antiretroviral agent ritonavir, which functions as an inhibitor of HIV protease. This compound has demonstrated significant biological activity in the modulation of HIV replication, contributing to its efficacy in the treatment of HIV infection and AIDS. Hydroxy ritonavir is primarily utilized in research applications aimed at understanding drug metabolism and the pharmacokinetics of HIV protease inhibitors.

Cat. No.

A70344

CAS No.

163217-74-1

2-Hydroxy atorvastatin lactone

2-Hydroxy atorvastatin lactone is a pharmacologically active metabolite of Atorvastatin, a potent HMG-CoA reductase inhibitor. This compound plays a significant role in lipid metabolism by effectively reducing cholesterol levels in the bloodstream. Its application is essential for research into lipid disorders and the pharmacokinetics of statin therapies.