1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2194
    Bergamottin
    Inhibitor 99.80%
    Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
    Bergamottin
  • HY-17459
    Clopidogrel hydrogen sulfate
    Inhibitor 99.43%
    Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation.Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor.
    Clopidogrel hydrogen sulfate
  • HY-16670
    Dafadine-A
    Inhibitor 98.94%
    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).
    Dafadine-A
  • HY-14273
    Isavuconazole
    Inhibitor 99.99%
    Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
    Isavuconazole
  • HY-N0370
    Bergapten
    Inhibitor 99.96%
    Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten
  • HY-125833
    Alpha-Naphthoflavone
    Inhibitor 98.54%
    Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.
    Alpha-Naphthoflavone
  • HY-N0693
    Schisandrin A
    Inhibitor 99.89%
    Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.
    Schisandrin A
  • HY-119293
    K777
    Inhibitor 99.77%
    K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
    K777
  • HY-19340
    TMS
    Inhibitor 98.61%
    TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity.
    TMS
  • HY-N0904
    Ginsenoside C-K
    99.92%
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K
  • HY-N0494
    Gentiopicroside
    Inhibitor 99.83%
    Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.
    Gentiopicroside
  • HY-B0725
    Doxepin Hydrochloride
    Inhibitor 99.79%
    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-131723
    Pregnenolone 16α-carbonitrile
    Activator 98.48%
    Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
    Pregnenolone 16α-carbonitrile
  • HY-134772
    AS1810722
    Inhibitor 98.14%
    AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.
    AS1810722
  • HY-N0043
    Ginsenoside Rd
    Inhibitor 99.88%
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
    Ginsenoside Rd
  • HY-W008364
    Olivetol
    Inhibitor 99.81%
    Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
    Olivetol
  • HY-17367A
    Atazanavir sulfate
    Inhibitor 99.94%
    Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
    Atazanavir sulfate
  • HY-U00448
    ADDA 5 hydrochloride
    Inhibitor ≥99.0%
    ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
    ADDA 5 hydrochloride
  • HY-N0482
    Phillyrin
    Activator 98.99%
    Phillyrin is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities. Phillyrin has potential inductive effects on rat CYP1A2 and CYP2D1 activities, without affecting CYP2C11 and CYP3A1/2 activities. Phillyrin has anti-influenza A virus activities.
    Phillyrin
  • HY-21065
    Tienilic acid
    99.85%
    Tienilic acid (Ticrynafen; ANP 3624) acts as a diuretic hypotensive agent. However, Tienilic acid induces hepatotoxicity. Tienilic acid is converted into electrophilic metabolites by cytochrome P450 (CYP) in vitro.
    Tienilic acid
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