1. Search Result
Search Result
Targets Recommended: Cytochrome P450
Results for "

Cytochrome P450

" in MCE Product Catalog:

79

Inhibitors & Agonists

2

Screening Libraries

4

Dye Reagents

25

Natural
Products

8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-B1184A
    (S)-Mephenytoin

    (+)-Mephenytoin

    Others Neurological Disease
    (S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism.
  • HY-16719
    Dapaconazole

    Cytochrome P450 Infection
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.
  • HY-B1151
    Climbazole

    BAY-e 6975

    Fungal Infection
    Climbazole (BAY-e 6975) is a potent antifungal agent. Climbazole also is a potent inducer of rat hepatic cytochrome P450.
  • HY-131452
    1-Ethynylpyrene

    Cytochrome P450 Cancer
    1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC50s of 0.18, 0.32, and 0.04 μM, respectively.
  • 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.
  • 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.
  • HY-15550
    4'-Hydroxy diclofenac

    Drug Metabolite Inflammation/Immunology Neurological Disease
    4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.
  • HY-103389
    1-Aminobenzotriazole

    ABT; 3-Aminobenzotriazole

    Cytochrome P450 Cancer
    1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).
  • HY-B1311
    Proadifen hydrochloride

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

    Cytochrome P450 Others
    Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM).
  • HY-111430
    1-Ethynylnaphthalene

    Cytochrome P450 Cancer
    1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
  • HY-112734
    4'-Methylchrysoeriol

    Cytochrome P450 Cancer
    4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
  • HY-B1307
    Zoxazolamine

    Others Neurological Disease
    Zoxazolamine is widely used for a pharmacologic test that serves as a convenient indicator of changes in cytochrome P-450 activity in rodents.
  • HY-100625
    BVT948

    Phosphatase Cytochrome P450 Histone Methyltransferase Cancer
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
  • HY-10882
    Clotrimazole

    Fungal Bacterial Autophagy Antibiotic Infection Cancer
    Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
  • HY-W011956
    6-Hydroxymelatonin

    Endogenous Metabolite Metabolic Disease Neurological Disease
    6-Hydroxymelatonin is a primary metabolic of Melatonin, which is metabolized by cytochrome P450 (CYP) 1A2.
  • HY-B1948
    Diniconazole

    Rac-diniconazole

    Bacterial Infection
    Diniconazole is a newly developed fungicide strongly inhibited lanosterol 14 alpha-demethylation catalyzed by a yeast cytochrome P-450.
  • HY-B1232
    Metyrapone

    Su-4885

    Cytochrome P450 Autophagy Metabolic Disease Cancer
    Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.
  • HY-14572
    PR-104A

    SN 27858

    DNA Alkylator/Crosslinker Cancer
    PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).
  • HY-14802
    Talarozole (R enantiomer)

    (R)-Talarozole

    Cytochrome P450 Cancer
    Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
  • HY-N2229
    Rhapontigenin

    Cytochrome P450 Fungal Bacterial Cancer Infection Inflammation/Immunology
    Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50  = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
  • HY-100638
    RPR132595A

    NPC

    Others Cancer
    RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
  • HY-B0873
    Uniconazole

    Cytochrome P450 Others
    Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki=68 nM), a family of enzymes that catabolize Abscisic acid, and thus, suppress gibberellin and sterol biosynthesis.
  • HY-117580
    16α-Hydroxyprednisolone

    OH-PRED

    Drug Metabolite Inflammation/Immunology
    16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes.
  • HY-30151
    Methoxsalen

    8-Methoxypsoralen; Xanthotoxin; 8-MOP

    Cytochrome P450 Inflammation/Immunology Cancer
    Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight.
  • HY-N6989
    Isoglycycoumarin

    Cytochrome P450 Metabolic Disease
    Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6).
  • HY-N1282
    Seneciphylline

    Gutathione S-transferase Cytochrome P450 Cancer
    Seneciphylline is a toxic pyrrolizidine alkaloid in Senecio plants. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities.
  • HY-N9508
    Perilla ketone

    Others Inflammation/Immunology
    Perilla ketone is a naturally occurring xenobiotic compound. Perilla ketone is activated by pulmonary P450 cytochrome enzymes in the lung, resulting in severe pulmonary damage and development of diffuse pulmonary edema.
  • HY-D0144
    Resorufin methyl ether

    Methoxyresorufin

    Cytochrome P450 Others
    Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate. Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents.
  • HY-N0688
    Linderane

    Cytochrome P450 Inflammation/Immunology
    Linderane, isolated from the root of Lindera strychnifolia, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.
  • HY-D0145
    7-Ethoxyresorufin

    Resorufin ethyl ether

    Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase.
  • HY-10493
    Cobicistat

    GS-9350

    Cytochrome P450 HIV Infection
    Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
  • HY-N6994
    Isoasatone A

    Others Infection
    Isoasatone A is a natural product isolated from the plant Heterotropa takaoi M., with anti-insect activity. Isoasatone A againsts S. litura by acting on cytochrome P450 monoxygenases and glutathione transferases.
  • HY-I0736
    Isonicotinic acid

    Drug Metabolite Endogenous Metabolite Others
    Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C.
  • HY-16670
    Dafadine-A

    Cytochrome P450 Others
    Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
  • HY-Y0110
    2-Naphthol

    Endogenous Metabolite Others
    2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
  • 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.
  • HY-D0147
    Resorufin pentyl ether

    Pentoxyresorufin

    Bacterial Infection
    Resorufin pentyl ether (Pentoxyresorufin) is a Resazurin (HY-111391) analogue. Resorufin pentyl ether can function as a substrate probe to characterize and differentiate between a variety of inducers of cytochromes P-450. Resorufin pentyl ether has bactericidal activity against N. gonorrhoeae.
  • HY-125598
    Secologanin

    Others Others
    Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin.
  • HY-134039
    5-Hydroxy-8-methoxypsoralen

    5-Hydroxyxanthotoxin

    Others Inflammation/Immunology
    5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite of Xanthotoxin. Xanthotoxin is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450), is an agent used to treat psoriasis, eczema, vitiligo and some cutaneous Lymphomas in conjunction with exposing the skin to sunlight.
  • HY-70013
    Abiraterone

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-129105
    Clomethiazole

    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.
  • HY-76200
    Voriconazole

    UK-109496

    Fungal Infection
    Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes.
  • HY-N2181
    Acetylshikonin

    Cytochrome P450 AChE Cancer Inflammation/Immunology
    Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity.
  • HY-N4205
    Tetrahydropiperine

    Cytochrome P450 Cancer
    Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum. Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM).
  • HY-W087919
    5-Methyl-2-furanmethanol

    Others Others
    5-Methyl-2-furanmethanol is a natural product that can be isolated from the essential oil of D. rupicola Biv.. 5-Methyl-2-furanmethanol also acts as a oxidative product of 2,5 dimethylfuran (DMF) by cytochrome P450 (CYP).
  • HY-B0876
    Fomepizole

    4-Methylpyrazole

    Cytochrome P450 Metabolic Disease
    Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.
  • HY-N5011
    5,7-Dimethoxyflavone

    Cytochrome P450 Cancer Inflammation/Immunology
    5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
  • HY-133116
    4-Hydroxyatomoxetine

    Others Neurological Disease
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
  • HY-15550S
    4'-Hydroxy diclofenac D4

    Drug Metabolite Inflammation/Immunology Neurological Disease
    4'-Hydroxy diclofenac D4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.
  • HY-106019C
    Liarozole dihydrochloride

    R75251 dihydrochloride

    Cytochrome P450 RAR/RXR Cancer Metabolic Disease Inflammation/Immunology
    Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.
  • HY-117010
    Kushenol K

    Cytochrome P450 HSV SGLT Infection Metabolic Disease
    Kushenol K, a flavonoid antioxidant isolated from the roots of Sophora flavescens. Kushenol K is a cytochrome P-450 3A4 (CYP3A4) inhibitor with a Ki value of 1.35 μM. Kushenol K shows weak antiviral activity against HSV-2 (EC50 of 147 μM). Kushenol K also inhibits the activity of SGLT1 and SGLT2.
  • HY-106019
    Liarozole

    R75251

    Cytochrome P450 RAR/RXR Cancer Metabolic Disease Inflammation/Immunology
    Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.
  • 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.
  • HY-N2574
    Gitogenin

    Glucosidase Metabolic Disease
    Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
  • 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.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
  • HY-17356
    Fenofibrate

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-13463
    Avatrombopag

    AKR-501; E5501; YM477

    Thrombopoietin Receptor Inflammation/Immunology
    Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
  • HY-13463B
    Avatrombopag hydrochloride

    AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride

    Thrombopoietin Receptor Cardiovascular Disease
    Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
  • HY-17514S
    Itraconazole-d5

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-N2425
    Rhodiosin

    AChE Metabolic Disease
    Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM.
  • HY-N0241
    Rhodionin

    AChE Metabolic Disease
    Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM. Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM.
  • HY-17356S
    Fenofibrate-d6

    PPAR Cytochrome P450 Autophagy Cardiovascular Disease Cancer
    Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
  • HY-133152
    Brexpiprazole S-oxide

    DM-3411

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • HY-B0845
    Prochloraz

    BTS 40542

    Fungal Estrogen Receptor/ERR Androgen Receptor Aryl Hydrocarbon Receptor Infection
    Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50=40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s=25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50=1 μM).
  • HY-B0847
    Propiconazole

    Fungal Reactive Oxygen Species Infection
    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).
  • HY-B0822
    Fipronil

    GABA Receptor Cytochrome P450 Neurological Disease
    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 (IC500s = 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.
  • HY-B0850
    Difenoconazole

    Fungal Infection
    Difenoconazole is a broad-spectrum triazole fungicide that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Difenoconazole inhibits the growth of F. graminearum isolates in vitro (EC50s=1.69-19.6 mg/L for mycelial growth). Difenoconazole also inhibits growth of A. sonali, F. fulva, B. cinerea, and R. solani (EC50s=0.131, 0.069, 0.297, and 0.252 mg/L, respectively).
  • HY-133152S
    Brexpiprazole S-oxide D8

    DM-3411 D8

    5-HT Receptor Dopamine Receptor Neurological Disease
    Brexpiprazole S-oxide D8 (DM-3411 D8) is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
  • 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-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).
  • HY-107204
    Furafylline

    Cytochrome P450 Cancer
    Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.
  • HY-N2071
    Cedrol

    (+)-Cedrol; α-Cedrol

    Cytochrome P450 Fungal Infection Inflammation/Immunology Cancer
    Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
  • HY-100902
    CDD3506

    Cytochrome P450 Metabolic Disease
    CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  • HY-100901
    CDD3505

    Cytochrome P450 Metabolic Disease
    CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
  • HY-B1751D
    Quinidine sulfate dihydrate

    Cytochrome P450 Cancer
    Quinidine sulfate dihydrate is a potent and selective inhibitor of cytochrome P450db and inhibits amphetamine metabolism in vivo. Quinidine sulfate dihydrate enhances the cytotoxicity of vincristine (VCR) in tumor cells and especially in VCR-resistant sublines of P388 leukemia (P388/VCR) and human myelogenous leukemia.
  • HY-117026
    LKY-047

    Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
  • HY-130494
    (±)11(12)-EET

    11,12-EET

    NOD-like Receptor (NLR) Inflammation/Immunology Cardiovascular Disease
    (±)11(12)-EET is a NLRP3 inflammasome inhibitor. (±)11(12)-EET can be used for the research of anti-inflammatory, angiogenic and cardioprotective.
  • HY-B1730
    Phensuximide

    Others Metabolic Disease Neurological Disease
    Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.