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Acetaminophen cyp450 Inhibitors

" in MCE Product Catalog:

54

Inhibitors & Agonists

21

Peptides

5

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-B0725S
    Doxepin D3 Hydrochloride

    		Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
  • HY-133091
    7-Ethoxycoumarin

    7-O-Ethylumbelliferone

    		 Cytochrome P450 Others
    7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
  • HY-133091S
    7-Ethoxycoumarin-d5

    		Isotope-Labeled Compounds Cytochrome P450 Others
    7-Ethoxycoumarin-d5 is deuterium labeled 7-Ethoxycoumarin. 7-Ethoxycoumarin is a substrate for cytochrome P450(CYP450) and has been used in the functional characterization of various CYPs[1].
  • HY-B0725
    Doxepin Hydrochloride

    		Histamine Receptor Cytochrome P450 Neurological Disease
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
  • HY-124527
    HET0016

    		Cytochrome P450 Cardiovascular Disease
    HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.
  • HY-109040
    Quilseconazole

    VT-1129

    		 Fungal Cytochrome P450 Infection
    Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
  • HY-N1407
    Polygalaxanthone III

    		Cytochrome P450 Inflammation/Immunology
    Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
  • HY-12594
    Paritaprevir

    ABT-450; Veruprevir

    		 HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor).
  • HY-12594A
    Paritaprevir dihydrate

    ABT-450 dihydrate; Veruprevir dihydrate

    		 HCV Protease HCV SARS-CoV Infection
    Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor).
  • HY-B0653
    Levobupivacaine

    (S)-(-)-Bupivacaine

    		 Sodium Channel Ferroptosis Cancer Neurological Disease
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-B0653A
    Levobupivacaine hydrochloride

    (S)-(-)-Bupivacaine monohydrochloride

    		 Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-N6023
    Thermopsoside

    		Cytochrome P450 Others
    Thermopsoside is a flavone derivative isolated from Aspalathus linearis. Thermopsoside exhibits inhibitory effects on CYP450 isozymes with IC50 values of 6.0 μM, 9.5 μM, 12.0 μM, 32.0 μM, for CYP3A4, CYP2C19, CYP2D6 and CYP2C9, respectively.
  • HY-101016
    17-ODYA

    		Cytochrome P450 Apoptosis Cardiovascular Disease
    17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes.
  • HY-G0004
    Acetaminophen metabolite 3-hydroxy-acetaminophen

    3-HydroxyAcetaminophen

    		 Drug Metabolite Inflammation/Immunology
    3-hydroxy-acetaminophen is a metabolite of Acetaminophen, which is a pain medicine.
  • HY-10965
    Rolofylline

    KW-3902

    		 Adenosine Receptor Neurological Disease
    Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.
  • HY-66006S
    4-Acetaminophen sulfate-d3

    		Isotope-Labeled Compounds Others
    4-Acetaminophen sulfate-d3 is the deuterium labeled 4-Acetaminophen sulfate[1].
  • HY-66006AS
    4-Acetaminophen sulfate-d3 potassium

    		Isotope-Labeled Compounds Others
    4-Acetaminophen sulfate-d3 (potassium) is the deuterium labeled 4-Acetaminophen sulfate potassium[1].
  • HY-66005S
    Acetaminophen-d4

    		COX Histone Acetyltransferase Endogenous Metabolite Inflammation/Immunology
    Acetaminophen-d4 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
  • HY-143911S
    Acetaminophen glucuronide-d3

    		Isotope-Labeled Compounds Others
    Acetaminophen glucuronide-d3 is the deuterium labeled Acetaminophen glucuronide[1].
  • HY-141736S
    Acetaminophen dimer-d6

    		Isotope-Labeled Compounds Others
    Acetaminophen dimer-d6 is the deuterium labeled Acetaminophen dimer[1].
  • HY-113083
    Acetaminophen glucuronide

    APAP-glu

    		 Drug Metabolite Endogenous Metabolite Others
    Acetaminophen glucuronide (APAP-glu) is an inactive glucuronide metabolite of Acetaminophen (HY-66005). Acetaminophen is a selective cyclooxygenase-2 (COX-2) inhibitor and a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
  • HY-66005
    Acetaminophen

    Paracetamol; 4-Acetamidophenol; 4'-Hydroxyacetanilide

    		 COX Histone Acetyltransferase Endogenous Metabolite Bacterial Parasite Inflammation/Immunology Cancer
    Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
  • HY-66005S2
    Acetaminophen-d7

    Paracetamol-d7; 4-Acetamidophenol-d7; 4'-Hydroxyacetanilide-d7

    		 Histone Acetyltransferase Endogenous Metabolite COX Inflammation/Immunology
    Acetaminophen-d7 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
  • HY-66005S1
    Acetaminophen-d3

    Paracetamol-d3; 4-Acetamidophenol-d3; 4'-Hydroxyacetanilide-d3

    		 COX Histone Acetyltransferase Endogenous Metabolite Inflammation/Immunology
    Acetaminophen-d3 is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
  • HY-P3690
    Ac-Leu-Leu-Norleucinol

    		Proteasome Others
    Ac-Leu-Leu-Norleucinol (ALLN) is a calpain inhibitor, can be used for research of Acetaminophen (HY-66005) induced acute liver damage, and lowers glutamic-oxalacetic transaminease (ALT) and glutamic-pyruvic transaminase (AST).
  • HY-135325
    4-Hydroxyacetophenone oxime

    		Drug Metabolite Inflammation/Immunology
    4-Hydroxyacetophenone oxime is an impurity of Acetaminophen (Paracetamol). Acetaminophen is a potent cyclooxygenase-2 (COX-2) and hepatic N-acetyltransferase 2 (NAT2) inhibitor, and used antipyretic and analgesic drug.
  • HY-124750
    NecroX-7

    		TNF Receptor Interleukin Related Toll-like Receptor (TLR) Reactive Oxygen Species Inflammation/Immunology Cardiovascular Disease
    NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.
  • HY-66004
    4-Acetamidophenyl acetate

    		Bacterial Parasite Inflammation/Immunology Cancer
    4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
  • HY-N2109
    Macranthoidin A

    		Others Metabolic Disease
    Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
  • HY-131349
    CCR4-351

    		CCR Cancer
    CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
  • HY-131349A
    CCR4-351 hydrochloride

    		CCR Cancer Metabolic Disease
    CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.
  • HY-W017464
    NAPQI

    		Endogenous Metabolite Metabolic Disease
    NAPQI is the toxic metabolite of Acetaminophen (HY-66005). NAPQI is also an inhibitor of enzymes in the vitamin K cycle. NAPQI is rapidly detoxified by glutathione (GSH), but in situations of GSH deficiency, excess NAPQI reacts with cysteine residues in proteins, causing cell death and toxicity in the liver.
  • HY-130419
    (±)13(14)-EpDPA

    13,14-EpDPE

    		 Others Neurological Disease Cardiovascular Disease
    (±)13(14)-EpDPA (13,14-EpDPE) is the product of the reaction of cytochrome P-450 epoxygenase with Docosahexaenoic Acid (DHA).(±)13(14)-EpDPA has antihyperalgesic and vasorelaxative activities.
  • HY-P1729
    M-2420

    		Fluorescent Dye Neurological Disease
    M-2420 is a fluorogenic substrate containing β-secretase site of the Swedish mutation of amyloid precursor protein (APP).
  • HY-113906A
    (αR,8aS)-GSK1614343

    		GHSR Inflammation/Immunology
    (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06.
  • HY-145733
    DI-1859

    		E1/E2/E3 Enzyme Cardiovascular Disease
    DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage.
  • HY-121983
    CAY10594

    		Phospholipase Cancer
    CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM). CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.
  • HY-P1016A
    BQ-3020 TFA

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    BQ-3020 (TFA) is a selective agonist of ETB receptor, inhibits [ 125I]ET-1 binding to ETB receptor with an IC50 of 0.2 nM in cerebellum, and causes vasoconstriction.
  • HY-126245
    Keap1-Nrf2-IN-1

    		Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injury.
  • HY-118607
    VU041

    		Potassium Channel Parasite Infection
    VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.
  • HY-N2023A
    Thalifendine chloride

    		Parasite Drug Metabolite Infection
    Thalifendine chloride is a metabolite of Berberine (HY-N0716), with antiplasmodial and antiamoebic activities. Thalifendine chloride shows activities against P. falciparum and E. histolytica with IC50s of 7.91 μM and 116 μM, respectively.
  • HY-P3255
    DA-JC4

    		Insulin Receptor Inflammation/Immunology Neurological Disease
    DA-JC4 is a dual GLP-1/GIP receptor agonist and can be used for the research of neurological disease and insulin signaling pathways.
  • HY-126245A
    Keap1-Nrf2-IN-1 TFA

    		Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1-Nrf2-IN-1 TFA (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 TFA activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
  • HY-P2161B
    TAK-683 acetate

    		Kisspeptin Receptor Cancer
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-P2161A
    TAK-683 TFA

    		Kisspeptin Receptor Cancer
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-P2161
    TAK-683

    		Kisspeptin Receptor Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
  • HY-P1206
    CH 275

    		Somatostatin Receptor Neurological Disease
    CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
  • HY-P3143
    BMSpep-57

    		PD-1/PD-L1 Cancer
    BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs.
  • HY-P3143A
    BMSpep-57 hydrochloride

    		PD-1/PD-L1 Cancer
    BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs.
  • HY-P0014
    Liraglutide

    		GCGR Metabolic Disease
    Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.
  • HY-P3066
    SKF 100398

    d(CH2)5Tyr(Et)VAVP

    		 Vasopressin Receptor Metabolic Disease
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.
  • HY-P0014S
    Liraglutide-d8 triTFA

    		Isotope-Labeled Compounds Others
    Liraglutide-d8 (triTFA) is the deuterium labeled Liraglutide (HY-P0014)[1].
  • HY-P3124
    BIM-23190

    		Somatostatin Receptor Cancer
    BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.
  • HY-P3124A
    BIM-23190 hydrochloride

    		Somatostatin Receptor Cancer
    BIM-23190 hydrochloride, a somatostatin analog, a selective SSRT2 and SSRT5 agonist, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.