Drug Metabolite

Cat. No.

A12600

CAS No.

239466-74-1

trans-R-138727

Trans-R-138727 is the trans isomer of R-138727, the active metabolite of the antiplatelet drug Prasugrel. It functions as an irreversible inhibitor of the P2Y12 receptor, effectively blocking ADP-induced platelet activation and aggregation. This compound serves as a valuable tool for research on platelet function and antithrombotic therapies. It can be utilized in studies aimed at understanding the mechanisms of platelet inhibition and cardiovascular disease management.

Cat. No.

A22660

CAS No.

34118-92-8

Acecainide HCl

Synonyms: N-Acetylprocainamide

Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion.

Cat. No.

A28659

CAS No.

2468202-15-3

O-Desmethyl dacomitinib

Synonyms: PF-05199265

O-Desmethyl dacomitinib is a significant metabolite of dacomitinib, functioning primarily as a pan-epidermal growth factor receptor (ErbB) tyrosine kinase inhibitor. Although it shows lower systemic exposure compared to its parent compound, its biological activity remains relevant for research into tumor biology and cancer therapeutics. O-Desmethyl dacomitinib's formation is closely linked to the enzymatic activity of CYP2D6, making it important for studies involving drug metabolism and pharmacogenomics.

Cat. No.

A31752

CAS No.

134612-80-9

3-O-Methyltolcapone

Synonyms: Ro 40-7591

3-O-Methyltolcapone is a drug metabolite derived from Tolcapone, a selective and potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 of 773 nM. This compound is known to block α-synuclein and Aβ42 oligomerization and fibrillogenesis, while also inducing oxidative stress, apoptosis in cancer cells, and reactive oxygen species (ROS) production. Research applications include studies related to cancer and neurological disorders, particularly in the context of Parkinson’s disease and neuroblastoma.

Cat. No.

A32952

CAS No.

204853-33-8

Tolcapone 3-β-D-glucuronide

Synonyms: Ro 61-1448

Tolcapone 3-β-D-glucuronide is a drug metabolite derived from Tolcapone, which serves as a selective and potent inhibitor of catechol-O-methyltransferase (COMT). While Tolcapone exhibits notable pharmacological activity, Tolcapone 3-β-D-glucuronide itself is pharmacologically inactive. Research indicates that Tolcapone plays a role in inhibiting α-synuclein and Aβ42 oligomerization, contributing to oxidative stress, cancer cell apoptosis, and reactive oxygen species (ROS) production. This metabolite is valuable for investigations into cancer mechanisms and neurological disorders, including Parkinson's disease and neuroblastoma.

Cat. No.

A33142

CAS No.

910297-58-4

Hydroxymethyl dasatinib

Hydroxymethyl dasatinib is a significant metabolite of Dasatinib, functioning primarily as a kinase inhibitor. It demonstrates biological activity with an IC50 of 46.7 nM in K562 chronic myeloid leukemia (CML) cells, indicating potent inhibitory effects on cell proliferation. This compound is applicable in research investigating the metabolic pathways of Dasatinib and its efficacy in targeting CML cells.

Cat. No.

A34773

CAS No.

18887-18-8

Hydroxytanshinone IIA

Hydroxytanshinone IIA is a hydroxylated metabolite of Tanshinone IIA, acting primarily through inhibition of angiogenesis. This compound targets the protein kinase domains of the vascular endothelial growth factor (VEGF) and its receptor VEGFR2, thereby modulating vascular processes. Hydroxytanshinone IIA is utilized in research focused on cancer biology, cardiovascular diseases, and therapeutic angiogenesis.

Cat. No.

A34869

CAS No.

835621-11-9

Regorafénib N-oxyde (M2)

Regorafénib N-oxyde (M2) is an active metabolite of Regorafenib, functioning as a multi-target inhibitor. It effectively targets VEGFR1/2/3, PDGFRβ, Kit, RET, and Raf-1, exhibiting IC50 values of 13, 4.2, 46, 22, 7, 1.5, and 2.5 nM, respectively. This compound is essential for studies involving cancer research and drug metabolism, providing insights into the pharmacological effects and therapeutic potential of Regorafenib.

Cat. No.

A36222

CAS No.

152831-00-0

6-Hydroxybenzbromarone

6-Hydroxybenzbromarone is a key metabolite of Benzbromarone, exhibiting enhanced pharmacological potency and a longer half-life. This compound functions as an inhibitor of the protein Eyes Absent 3 (EYA3), with an IC50 of 21.5 μM. Its anti-angiogenic properties are evidenced by its ability to inhibit cell migration, tubulogenesis, and angiogenic sprouting, making it a valuable reagent for research in cancer biology and vascular development.

Cat. No.

A38465

CAS No.

1445383-14-1

ALS-8112-TP

ALS-8112-TP is the 5'-triphosphate metabolite of ALS-8112, acting as a selective and competitive inhibitor of respiratory syncytial virus (RSV) RNA polymerase. This compound specifically targets the RSV polymerase complex, leading to chain termination during RNA synthesis, while exhibiting selectivity against other unrelated viral and host polymerases such as that of hepatitis C virus (HCV). ALS-8112-TP is valuable for research applications focused on RSV infection mechanisms and antiviral therapeutic development.

Cat. No.

A39680

CAS No.

757220-04-5

Di-N-desethyl amiodarone hydrochloride

Di-N-desethyl amiodarone hydrochloride is a metabolite of amiodarone that acts as a potent inhibitor of the respiratory chain. Its biological activity makes it valuable for studying mitochondrial function and cellular respiration. This reagent can be utilized in research applications focusing on cardiology and toxicology, particularly in the investigation of drug metabolism and potential therapeutic effects.

Cat. No.

A41818

CAS No.

139755-82-1

N-Desmethyl Sildenafil

Synonyms: Desmethylsildenafil; UK-103,320

N-Desmethyl Sildenafil is an active metabolite of the well-known phosphodiesterase type 5 (PDE5) inhibitor, Sildenafil. This compound retains significant biological activity, contributing to the vasodilatory effects associated with PDE5 inhibition. Research applications include studies on erectile dysfunction and pulmonary hypertension, as well as the investigation of metabolic pathways involving Sildenafil.

Cat. No.

A42141

CAS No.

2656442-91-8

Avanafil metabolite M4

Avanafil metabolite M4 is a primary active metabolite of the selective phosphodiesterase-5 (PDE-5) inhibitor, Avanafil. It targets PDE-5 and exhibits significant biological activity by inhibiting cGMP hydrolysis, leading to increased cGMP levels which activates the NO/cGMP/PKG signaling pathway. This metabolite is relevant for research applications in the context of erectile dysfunction and osteoporosis, as it helps to mitigate bone mineral density loss, bone atrophy, and oxidative stress.

Cat. No.

A48160

CAS No.

117977-21-6

Rabeprazole Sulfide

Rabeprazole Sulfide is a sulfide metabolite of the proton pump inhibitor Rabeprazole. It exhibits inhibitory effects on the motility of Helicobacter pylori, making it a valuable tool for studying this bacterial infection. Research utilizing Rabeprazole Sulfide can contribute to a better understanding of Helicobacter pylori's role in gastrointestinal diseases.

Cat. No.

A48286

CAS No.

108656-33-3

Florfenicol amine hydrochloride

Florfenicol amine hydrochloride is a metabolite of Florfenicol, functioning primarily as an inhibitor of bacterial protein synthesis. It exerts its effects by binding to the 50S and 70S ribosomal subunits, disrupting peptidyltransferase activity. This compound plays a crucial role in the study of antibiotic action and resistance mechanisms and is particularly relevant for research focused on bacterial infections in aquaculture settings.

Cat. No.

A58126

CAS No.

92264-81-8

Hydroxybupropion

Hydroxybupropion is the primary active metabolite of the atypical antidepressant and smoking-cessation agent bupropion. It is primarily metabolized by the CYP2B6 enzyme and functions as an inhibitor of norepinephrine uptake, with an IC50 value of 1.7 μM. Additionally, hydroxybupropion acts as an antagonist at nicotinic acetylcholine receptors, contributing to its pharmacological profile. This compound serves as a valuable tool in research exploring depression, smoking cessation, and the pharmacokinetics of bupropion-derived therapies.

Cat. No.

A64276

CAS No.

52807-12-2

4'-Hydroxy flurbiprofen

4'-Hydroxy flurbiprofen is an oxidative metabolite of flurbiprofen, resulting from the activity of the cytochrome P450 enzyme system. This compound exhibits significant biological activity as a potent inhibitor of cyclooxygenase-1 (COX-1), achieving a 94% inhibition rate at a concentration of 1000 µM. Its research applications include studies on analgesic mechanisms and the exploration of anti-inflammatory pathways.

Cat. No.

A64285

CAS No.

170571-01-4

Celecoxib carboxylic acid

Celecoxib carboxylic acid is a metabolite of celecoxib, a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 40 nM. This compound serves as a valuable tool for studying the pharmacokinetics and metabolism of celecoxib in biological systems. It is applicable in research focused on inflammation, pain management, and cancer therapies, facilitating insights into drug action and therapeutic efficacy.

Cat. No.

A64300

CAS No.

52079-10-4

(S)-6-O-Desmethylnaproxen

Synonyms: (S)-6-Desmethyl Naproxen

(S)-6-O-Desmethylnaproxen is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor (+)-naproxen, formed through the action of cytochrome P450 isoforms CYP1A2 and CYP2C9. This compound plays a significant role in pharmacokinetic studies and serves as a valuable tool for researchers investigating drug metabolism and interactions. Its biological activity is central to understanding the pharmacological effects and potential side effects associated with naproxen therapy.

Cat. No.

A64563

CAS No.

76690-94-3

(±)-Ketoprofen glucuronide

(±)-Ketoprofen glucuronide is a glucuronide metabolite of the anti-inflammatory drug ketoprofen, primarily acting through inhibition of cyclooxygenase enzymes. This compound is integral for understanding the pharmacokinetics and metabolic pathways of NSAIDs in biochemical research. It serves as a valuable tool in studies related to drug metabolism, efficacy, and safety profiles of non-steroidal anti-inflammatory agents.

Cat. No.

A65807

CAS No.

871701-87-0

GSK1790627

GSK1790627 is the N-deacetylated metabolite of Trametinib, a potent and selective MEK inhibitor. This compound exhibits biological activities that include the activation of autophagy and the induction of apoptosis in tumor cells. GSK1790627 is instrumental in research focused on cancer treatment and the mechanistic understanding of MEK pathway modulation.

Cat. No.

A67643

CAS No.

357399-43-0

Bupropion morpholinol

Bupropion morpholinol, a primary metabolite of Bupropion, serves as an inhibitor of the dopamine and norepinephrine transporters, as well as the α4β2 nicotinic receptor in vitro. This compound is important for research into its antidepressant properties and mechanisms involved in smoking cessation. Its biological activity underlines the role of Bupropion morpholinol in neurotransmitter modulation and highlights its relevance in neuropharmacology studies.

Cat. No.

A68363

CAS No.

127780-16-9

Pantoprazole sulfone

Pantoprazole sulfone is a metabolite of the gastric H+/K+ ATPase pump inhibitor, Pantoprazole. This compound is crucial for studying the pharmacokinetics and biochemical pathways of Pantoprazole metabolism. Research applications include exploring its role in acid-related disorders and evaluating its influence on drug interactions in gastric physiology.

Cat. No.

A68376

CAS No.

103876-98-8

4-Hydroxy omeprazole sulfide

4-Hydroxy omeprazole sulfide is a key metabolite of the proton pump inhibitor omeprazole, primarily involved in modifying gastric acid secretion. This compound serves as a valuable tool in pharmacokinetic and metabolic studies of omeprazole and its effects on gastric mucosa. Its biological activity is significant for understanding drug metabolism and potential drug interactions in gastrointestinal research.

Cat. No.

A69912

CAS No.

152503-50-9

Diosmetin-3-O-glucuronide

Diosmetin-3-O-glucuronide is a principal metabolite of Diosmetin, functioning primarily as an inhibitor of the human CYP1A enzyme. This glucuronide conjugate plays an essential role in studying the pharmacokinetics and bioactivity of flavonoids. Its presence in plasma and urine makes it valuable for research applications focused on metabolic pathways and the therapeutic effects of flavonoid compounds.