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CYP450

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38

Inhibitors & Agonists

10

Natural
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3

Isotope-Labeled Compounds

1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0725S

    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].
    Doxepin D3 Hydrochloride
  • HY-153671

    Others Infection
    4'-Methyl-β-naphthoflavone is a metabolite of Naphthoflavones (benzoflavones) in fungal. Naphthoflavones are activators or inhibitors of CYP-450 .
    4'-Methyl-β-naphthoflavone
  • HY-133091

    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].
    7-Ethoxycoumarin
  • HY-Z0056S

    pentadeuterobromobenzene

    Cytochrome P450 Endocrinology
    Bromobenzene-d5 is the deuterium labeled Bromobenzene. Bromobenzene is a well-known environmental toxin which causes liver and kidney damage through CYP450-mediated bio-activation to generate reactive metabolites and, consequently, oxidative stress[1].
    Bromobenzene-d5
  • HY-B0725
    Doxepin Hydrochloride
    4 Publications Verification

    Histamine Receptor Cytochrome P450 Neurological Disease Cancer
    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 .
    .
    Doxepin Hydrochloride
  • HY-157170

    Cytochrome P450 Cancer
    CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450 .
    CYP450-IN-1
  • HY-130550

    Endogenous Metabolite Others
    (±)7(8)-EpDPA is an epoxide derivative of docosahexaenoic acid (DHA) metabolized by CYP450 .
    (±)7(8)-EpDPA
  • HY-145546

    Cytochrome P450 Metabolic Disease
    14(15)-EpETE is the epoxide of cytochrome P450 (CYP450) and is involved in the regulation of vascular tone and renal function .
    14(15)-EpETE
  • HY-133091S

    Cytochrome P450 Isotope-Labeled Compounds 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].
    7-Ethoxycoumarin-d5
  • HY-130219

    Endogenous Metabolite Others
    18-HETE (compound 3) is a monooxygenase metabolite of cytochrome P450 (CYP450).18- HETE consists of arachidonic acid bearing a hydroxy substituent at position 18 .
    18-HETE
  • HY-124527
    HET0016
    2 Publications Verification

    Cytochrome P450 Cardiovascular Disease Cancer
    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 .
    HET0016
  • HY-109040

    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 .
    Quilseconazole
  • HY-148907

    CaMK MEK Mixed Lineage Kinase Cancer
    CS640 is a selective inhibitor of calmodulin-dependent kinases. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, PIP5K1C, MEK5, RIPK4 and MLK3 with IC50 values of 0.08, 0.03, 0.001, 0.001, 11.2, 0.025, 5.69 and 2.75 μM, respectively. CS640 also shows inhibitory effects to CYP450 2C9 and CYP450 2C19 with IC50 values of 6 and 10 μM, respectively .
    CS640
  • HY-115493

    CXCR Others
    TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca 2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM .
    TIQ-15
  • HY-N1407

    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 .
    Polygalaxanthone III
  • HY-B0725R

    Histamine Receptor Cytochrome P450 Neurological Disease Cancer
    Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. 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 .
    .
    Doxepin Hydrochloride (Standard)
  • HY-W803860

    Drug Metabolite Sodium Channel Cardiovascular Disease
    N-Depropylpropafenone is an active metabolite of Propafenone (HY-B0432), generated through the CYP450 enzyme system (mainly CYP2D6). It functions by blocking sodium ion channels, slowing myocardial conduction and exhibiting certain antiarrhythmic effects .
    N-Depropylpropafenone
  • HY-113482

    1β-OH-DCA

    Endogenous Metabolite Cytochrome P450 Metabolic Disease
    1β-Hydroxydeoxycholic acid (1β-OH-DCA), a secondary bile acid, is a CYP3A biomarker. Deoxycholic acid is specifically metabolized into 1β-Hydroxydeoxycholic acid by CYP3A4 and CYP3A7 using recombinant human CYP450 enzymes .
    1β-Hydroxydeoxycholic acid
  • HY-12594
    Paritaprevir
    Maximum Cited Publications
    12 Publications Verification

    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) .
    Paritaprevir
  • HY-12594A

    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) .
    Paritaprevir dihydrate
  • HY-164049

    Prostaglandin Receptor Inflammation/Immunology
    TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases .
    TG8-260
  • HY-N1407R

    Cytochrome P450 Inflammation/Immunology
    Polygalaxanthone III (Standard) is the analytical standard of Polygalaxanthone III. This product is intended for research and analytical applications. 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 .
    Polygalaxanthone III (Standard)
  • HY-B0653A
    Levobupivacaine hydrochloride
    2 Publications Verification

    (S)-(-)-Bupivacaine monohydrochloride

    Sodium Channel Ferroptosis Cardiovascular Disease Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. 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 .
    Levobupivacaine hydrochloride
  • HY-B0653

    (S)-(-)-Bupivacaine

    Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. 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 .
    Levobupivacaine
  • HY-N6023

    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 .
    Thermopsoside
  • HY-130309

    (±)8,9-EEQ; (±)8,9-epoxy Eicosatetraenoic acid

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Eicosapentaenoic acid (EPA) is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE, relaxes vascular and airway smooth muscle by activating large conductance Ca 2+-activated K + (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo.
    (±)8(9)-EpETE
  • HY-30152
    Xanthotoxol
    2 Publications Verification

    8-Hydroxypsoralen

    5-HT Receptor Reactive Oxygen Species Endogenous Metabolite Neurological Disease Inflammation/Immunology
    Xanthotoxol (8-Hydroxypsoralen) It is a kind of fragrant bean substance, and it is a CYP450 inhibitor. Xanthotoxol has anti-inflammatory, anti-inflammatory, and 5-HT antagonistic and protective effects. Xanthotoxol inhibited CYP3A4 sum CYP1A2 IC50s separation 7.43 μM sum 27.82 μM. Xanthotoxol can pass through MAPK and NF-κB, inhibiting inflammation .
    Xanthotoxol
  • HY-30152R

    5-HT Receptor Reactive Oxygen Species Endogenous Metabolite Neurological Disease Inflammation/Immunology
    Xanthotoxol (Standard) is the analytical standard of Xanthotoxol. This product is intended for research and analytical applications. Xanthotoxol (8-Hydroxypsoralen) It is a kind of fragrant bean substance, and it is a CYP450 inhibitor. Xanthotoxol has anti-inflammatory, anti-inflammatory, and 5-HT antagonistic and protective effects. Xanthotoxol inhibited CYP3A4 sum CYP1A2 IC50s separation 7.43 μM sum 27.82 μM. Xanthotoxol can pass through MAPK and NF-κB, inhibiting inflammation .
    Xanthotoxol (Standard)
  • HY-10965

    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 .
    Rolofylline
  • HY-101016

    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 . 17-ODYA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    17-ODYA
  • HY-N2071
    Cedrol
    1 Publications Verification

    (+)-Cedrol; α-Cedrol

    Cytochrome P450 Fungal Apoptosis Caspase Platelet-activating Factor Receptor (PAFR) Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties .
    Cedrol
  • HY-131349

    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 .
    CCR4-351
  • HY-131349A

    CCR Metabolic Disease Cancer
    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 .
    CCR4-351 hydrochloride
  • HY-N2071R

    Cytochrome P450 Fungal Apoptosis Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    Cedrol (Standard) is the analytical standard of Cedrol. This product is intended for research and analytical applications. Cedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
    Cedrol (Standard)
  • HY-130419

    13,14-EpDPE

    Others Cardiovascular Disease Neurological 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 .
    (±)13(14)-EpDPA
  • HY-113906A

    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 .
    (αR,8aS)-GSK1614343
  • HY-118607

    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 .
    VU041
  • HY-161350

    Anaplastic lymphoma kinase (ALK) HDAC Cancer
    ALK/HDAC-IN-1 is a dual inhibitor for ALK and HDAC6, with IC50s of 16 nM and 1.03 μM, respectively. ALK/HDAC-IN-1 exhibits antitumor activity .
    ALK/HDAC-IN-1

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