2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Drug Metabolite

Drug Metabolite

Drug Metabolite

Related Products

PDF 3.95 MB

Drug metabolite results when a drug is metabolized into a modified form which continues to produce effects. Drug metabolism redox reactions such as heteroatom dealkylations, hydroxylations, heteroatom oxygenations, reductions, and dehydrogenations can yield active metabolites, and in rare cases even conjugation reactions can yield an active metabolite.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18719
    Endoxifen (Z-isomer)
    		99.19%
    Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer inhibits PKCβ1 kinase activity. Endoxifen Z-isomer attenuates PKCβ1-activated AKTSer473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer exhibits anticancer activity against hormone-resistant metastatic breast cancer.
    Endoxifen (Z-isomer)
  • HY-G0021
    N-Desmethylclozapine
    		99.10%
    N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
    N-Desmethylclozapine
  • HY-103638S
    3-Methoxytyramine-d4 hydrochloride
    		98.66%
    3-Methoxytyramine-d4 (hydrochloride) is the deuterium labeled 3-Methoxytyramine hydrochloride. 3-Methoxytyramine hydrochloride is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1).
    3-Methoxytyramine-d<sub>4</sub> hydrochloride
  • HY-100750
    Norverapamil hydrochloride
    		99.80%
    Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
    Norverapamil hydrochloride
  • HY-113289
    Brassicasterol
    		99.93%
    Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacterium tuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease.
    Brassicasterol
  • HY-N2481
    Oroxylin A-7-O-glucuronide
    		99.83%
    Oroxylin A-7-O-glucuronide (oroxyloside) is an orally active flavonoid glucuronide and metabolite of Oroxylin A (HY-N0560). Oroxylin A-7-O-glucuronide can be extracted from the dried root of Scutellaria baicalensis. Oroxylin A-7-O-glucuronide exhibits prolyl oligopeptidase inhibitory activity. Oroxylin A-7-O-glucuronide inhibits the JNK pathway, upregulates PPARγ, and inhibits NF-κB p65 nuclear translocation. Oroxylin A-7-O-glucuronide reduces cytokine (IL-1β, IL-6) production. Oroxylin A-7-O-glucuronide exhibits anti-angiogenic, anti-tumor (glioma, liver cancer), anti-inflammatory, and hepatoprotective activities.
    Oroxylin A-7-O-glucuronide
  • HY-W052508
    Norquetiapine
    		99.95%
    Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.
    Norquetiapine
  • HY-114794
    Desglymidodrine
    Desglymidodrine (ST 1059), the active metabolite of Midodrine(HY-12749), is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure.
    Desglymidodrine
  • HY-129099A
    N-Desmethyltamoxifen hydrochloride
    		99.63%
    N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
    N-Desmethyltamoxifen hydrochloride
  • HY-B1398
    Ampyrone
    		99.72%
    Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy.
    Ampyrone
  • HY-114988
    PGE-M
    		99.9%
    PGE-M (tetranor-PGEM) is a metabolite of Prostaglandin E2 (HY-101952) and also an inflammatory biomarker. Urinary PGE-M is a potential biomarker for detecting advanced colorectal tumors. PGE-M can be used in studies related to colorectal cancer, obesity, aging and breast cancer.
    PGE-M
  • HY-W391635
    3-Oxo deoxycholic acid
    		99.88%
    3-oxo Deoxycholic acid is a secondary bile acid and a metabolite of Deoxycholic acid (HY-N0593) in C. perfringens.
    3-Oxo deoxycholic acid
  • HY-W013378
    Carbamazepine 10,11-epoxide
    		99.14%
    Carbamazepine 10,11-epoxide is a metabolite of Carbamazepine (HY-B0246). Carbamazepine 10,11-epoxide can be used to monitor for Carbamazepine.
    Carbamazepine 10,11-epoxide
  • HY-W013272
    Hydroxyflutamide
    		99.77%
    Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC50 of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.
    Hydroxyflutamide
  • HY-15157
    Calcitetrol
    		99.94%
    Calcitetrol (1α, 24, 25-Trihydroxy VD3), a Vitamin D3 (HY-15398) metabolite, is the hormonally active form of vitamin D. Calcitetrol participates in regulation of Treg cells. Calcitetrol can be used for the research of Toxoplasma gondii infection.
    Calcitetrol
  • HY-135391
    Ezetimibe phenoxy glucuronide
    		99.77%
    Ezetimibe phenoxy glucuronide (Ezetimibe glucuronide) is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.
    Ezetimibe phenoxy glucuronide
  • HY-108251
    Methotrexate metabolite
    		98.44%
    Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation.
    Methotrexate metabolite
  • HY-N2013
    Aristolactam I
    		99.44%
    Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis.
    Aristolactam I
  • HY-N3995
    5β-Dihydrocortisol
    		99.86%
    5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis.
    5β-Dihydrocortisol
  • HY-113121R
    Vanillylmandelic acid (Standard)
    Vanillylmandelic acid (Standard) is the analytical standard of Vanillylmandelic acid. This product is intended for research and analytical applications. Vanillylmandelic acid is the endproduct of epinephrine and norepinephrine metabolism. Vanillylmandelic acid can be used as an indication of the disorder in neurotransmitter metabolism as well. Vanillylmandelic acid has antioxidant activity towards DPPH radical with an IC50 value of 33 μM.
    Vanillylmandelic acid (Standard)
Cat. No. Product Name / Synonyms Application Reactivity