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liver cytochrome

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39

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7

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9

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100386
    Ticlopidine
    1 Publications Verification

    PCR 5332

    		 Cytochrome P450 Cardiovascular Disease
    Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
    Ticlopidine
  • HY-B1311
    Proadifen hydrochloride
    1 Publications Verification

    SKF-525A; U-5446; RP-5171

    		 Cytochrome P450 Monoamine Oxidase Bcl-2 Family Survivin PARP Neurological Disease Inflammation/Immunology Cancer
    Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
    Proadifen hydrochloride
  • HY-N8094
    Kushenol M

    		Cytochrome P450 Others
    Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
    Kushenol M
  • HY-121385
    Hydroxy bosentan

    Ro 48-5033

    		 Endogenous Metabolite Cardiovascular Disease
    Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities .
    Hydroxy bosentan
  • HY-100386R
    Ticlopidine (Standard)

    		Cytochrome P450 Cardiovascular Disease
    Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
    Ticlopidine (Standard)
  • HY-118167
    Monoethylglycinexylidide

    		Drug Metabolite Metabolic Disease Inflammation/Immunology
    Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver [1] .
    Monoethylglycinexylidide
  • HY-W099331
    Monoethylglycinexylidide hydrochloride

    MEGX hydrochloride; Norlidocaine hydrochloride

    		 Drug Metabolite Metabolic Disease Inflammation/Immunology
    Monoethylglycinexylidide (MEGX) hydrochloride is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver. Monoethylglycinexylidide has proven to be a highly sensitive indicator of hepatic dysfunction, especially in the field of liver transplantation .
    Monoethylglycinexylidide hydrochloride
  • HY-118167R
    Monoethylglycinexylidide (Standard)

    		Drug Metabolite Metabolic Disease Inflammation/Immunology
    Monoethylglycinexylidide (Standard) is the analytical standard of Monoethylglycinexylidide. This product is intended for research and analytical applications. Monoethylglycinexylidide is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver .
    Monoethylglycinexylidide (Standard)
  • HY-119536
    Norsufentanil

    		Others Neurological Disease
    Sufentanil is a potent synthetic opioid analgesic. Norsufentanil, a metabolite of sufentanil, is produced by the oxidative N-dealkylation of the liver cytochrome P450 isomer. Norsufentanil has analgesic activity .
    Norsufentanil
  • HY-137580
    N-Desmethyl Eletriptan

    		Others Metabolic Disease
    N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes.
    N-Desmethyl Eletriptan
  • HY-B1311R
    Proadifen hydrochloride (Standard)

    		Cytochrome P450 Monoamine Oxidase Bcl-2 Family Survivin PARP Neurological Disease Inflammation/Immunology Cancer
    Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
    Proadifen hydrochloride (Standard)
  • HY-145490
    trans-Hydroxy Glimepiride

    		Others Metabolic Disease
    trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea Glimepiride (HY-B0104). It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9.
    trans-Hydroxy Glimepiride
  • HY-B0476
    Phenacetin

    Acetophenetidin

    		 COX Inflammation/Immunology
    Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin
  • HY-116444A
    16-HETE

    		Na+/K+ ATPase Cardiovascular Disease Inflammation/Immunology
    16-HETE is arachidonic acid metabolite through subterminal hydroxylation by cytochrome P-450. 16-HETE exhibits vasodilatory and PMN inhibitory effects and serves as biomarker for early stages of non-alcoholic fatty liver disease .
    16-HETE
  • HY-129105
    Clomethiazole
    2 Publications Verification

    		 GABA Receptor Cytochrome P450 Neurological Disease
    Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
    Clomethiazole
  • HY-B1351
    Bilberry Extract

    		Others Metabolic Disease
    Bilberry Extract is a bilberry extract, and its components include: Anthocyanidins. Bilberry Extract has potential antioxidant activity and can regulate specific metabolic enzymes in the liver, such as cytochrome P450 (CYP) 2C11 and CYP2E1 involved in drug metabolism. .
    Bilberry Extract
  • HY-129491S
    O-Desmethyl Midostaurin-d5

    CGP62221-d5; O-Desmethyl PKC412-d5

    		 Isotope-Labeled Compounds Drug Metabolite Cancer
    O-Desmethyl Midostaurin-d5 is a deuterium labeled O-Desmethyl PKC412. O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism[1].
    O-Desmethyl Midostaurin-d5
  • HY-121385S
    Hydroxy Bosentan-d6

    Ro 48-5033-d6

    		 Isotope-Labeled Compounds Endogenous Metabolite Cardiovascular Disease
    Hydroxy Bosentan-d6 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
    Hydroxy Bosentan-d6
  • HY-121385S1
    Hydroxy Bosentan-d4

    Ro 48-5033-d4

    		 Isotope-Labeled Compounds Endogenous Metabolite Cardiovascular Disease
    Hydroxy Bosentan-d4 is deuterium labeled Hydroxy bosentan. Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Ro 48-5033 assists BOS pharmacologically, retaining 10%-20% activities[1].
    Hydroxy Bosentan-d4
  • HY-B0476S
    Phenacetin-d5

    Acetophenetidin-d5

    		 COX Inflammation/Immunology
    Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
    Phenacetin-d5
  • HY-113111
    11,12-DiHETrE

    		Endogenous Metabolite Inflammation/Immunology
    11,12-DiHETrE, an endogenous metabolite, is a Cytochrome P450 (P450) eicosanoid. 11,12-DiHETrE can be used for preterm labor research. 11,12-DiHETrE can be used as a single biomarker for differentiating NAFL (nonalcoholic fatty liver) from NASH (nonalcoholic steatohepatitis) .
    11,12-DiHETrE
  • HY-B0476S1
    Phenacetin-13C

    		COX Inflammation/Immunology
    Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
    Phenacetin-13C
  • HY-B0476R
    Phenacetin (Standard)

    Acetophenetidin (Standard)

    		 COX Inflammation/Immunology
    Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
    Phenacetin (Standard)
  • HY-160979
    Bisfentidine

    DA-5047

    		 Histamine Receptor Others Endocrinology
    Bisfentidine is an H2 receptor antagonist, Bisfentidine can block the H2 receptor on the cells of the stomach wall, and reduce the secretion of stomach acid. Bisfentidine binds to cytochrome P-450 in liver microsomes and affects drug metabolism. Bisfentidine can be used in the study of metabolic processes of drugs, lipid peroxidation processes and peptic ulcers diseases .
    Bisfentidine
  • HY-N2181
    Acetylshikonin
    1 Publications Verification

    		 Cytochrome P450 Apoptosis Bacterial Autophagy Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD) .
    Acetylshikonin
  • HY-129491
    O-Desmethyl Midostaurin

    CGP62221; O-Desmethyl PKC412

    		 PKC Cancer
    O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo . Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
    O-Desmethyl Midostaurin
  • HY-135390
    Hydroxy desmethyl Bosentan

    Ro 64-1056

    		 Drug Metabolite Cardiovascular Disease
    Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
    Hydroxy desmethyl Bosentan
  • HY-113031
    16a-Hydroxydehydroisoandrosterone

    16α-Hydroxy-DHEA; 16α-OH-DHEA; 16α-hydroxy DHEA

    		 Others Endocrinology
    16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
    16a-Hydroxydehydroisoandrosterone
  • HY-113777
    22-HDHA

    22-Hydroxy Docosahexaenoic acid; 22-OH DHA

    		 Others Metabolic Disease
    22-HDHA is an oxidation product of docosahexaenoic acid.1 In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
    22-HDHA
  • HY-N7454
    Anhydroerythromycin A

    		Antibiotic Bacterial Infection
    Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
    Anhydroerythromycin A
  • HY-125904
    4-Hydroxyretinoic acid

    		RAR/RXR Neurological Disease Inflammation/Immunology Cancer
    4-Hydroxyretinoic acid (4-HRA) is a naturally occurring retinoid derivative with diverse biological effects. 4-Hydroxyretinoic acid is formed from retinol catalyzed by cytochrome P-450 isozyme(s), and is mainly metabolized by the liver in the body. 4-Hydroxyretinoic acid also serves as the substrate for human liver microsomal UDP-glucuronosyltransferase(s) and recombinant UGT2B7. 4-Hydroxyretinoic acid regulates gene expression and cell differentiation via binding to nuclear receptor RAR (Retinoic Acid Receptor), and activates RARs and RXR-alpha, to induce cancer cell apoptosis. In addition, 4-Hydroxyretinoic acid is also involved in various physiological processes such as immune regulation, neuroprotection, and anti-oxidation .
    4-Hydroxyretinoic acid
  • HY-N7454R
    Anhydroerythromycin A (Standard)

    		Antibiotic Bacterial Infection
    Anhydroerythromycin A (Standard) is the analytical standard of Anhydroerythromycin A. This product is intended for research and analytical applications. Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
    Anhydroerythromycin A (Standard)
  • HY-169119
    Antifungal agent 114

    		Cytochrome P450 Fungal Infection
    Antifungal agent 114 (Compound 19g) is an inhibitor for Cytochrome P450, that inhibits CYP1A2, CYP2C9, CYP2C19 CYP2D6 and CYP3A4 at 10 μM. Antifungal agent 114 exhibits antifungal activity against Cryptococcus neoformans, Candida and Aspergillus, with MIC <0.0625 μg/mL. Antifungal agent 114 exhibits good metabolic stability in human liver microsomes with a half-time of 107 minutes .
    Antifungal agent 114
  • HY-100386S
    Ticlopidine-d4

    PCR 5332-d4

    		 Isotope-Labeled Compounds Cytochrome P450 Cardiovascular Disease
    Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
    Ticlopidine-d4
  • HY-B0847S
    Propiconazole-d7

    		Fungal Reactive Oxygen Species Infection
    Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].
    Propiconazole-d7
  • HY-B0847S1
    Propiconazole-d3 nitrate

    		Fungal Reactive Oxygen Species Infection
    Propiconazole-d3 (nitrate) is the deuterium labeled Propiconazole nitrate. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS).
    Propiconazole-d3 nitrate
  • HY-B0822S1
    Fipronil-13C6

    		GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-N6972
    Cepharanthine
    4 Publications Verification

    		 Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
    Cepharanthine
  • HY-N6972R
    Cepharanthine (Standard)

    		Autophagy SARS-CoV Cytochrome P450 Apoptosis Parasite Infection Inflammation/Immunology Cancer
    Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
    Cepharanthine (Standard)

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