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-A0069S
    Doxylamine-d5 succinate
    Activator ≥98.0%
    Doxylamine-d5 succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia.
    Doxylamine-d<sub>5</sub> succinate
  • HY-119578
    Imiprothrin
    Activator
    Imiprothrin is an inducer that induces CYP1A2 and metallothionein 1a, with significant genotoxicity and cytotoxicity. In rat hepatocytes, Imiprothrin initiates detoxification responses by triggering the overexpression of these two genes. Imiprothrin induces chromosomal aberrations and micronucleus formation in rat bone marrow cells, and causes DNA damage in hepatocytes. Imiprothrin triggers oxidative stress in rats, leading to lipid peroxidation, excessive reactive oxygen species production and redox imbalance, which in turn impairs liver and kidney functions and causes tissue damage. Imiprothrin inhibits weight gain in mice, and even causes high mortality in female mice at high doses. However, it shows no carcinogenicity in rat experiments; among relevant indicators, aspartate aminotransferase and total protein are identified as sensitive toxicity biomarkers.
    Imiprothrin
  • HY-D0092R
    7-Ethoxy-4-methylcoumarin (Standard)
    7-Ethoxy-4-methylcoumarin (Standard) is the analytical standard of 7-Ethoxy-4-methylcoumarin. This product is intended for research and analytical applications. 7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6.
    7-Ethoxy-4-methylcoumarin (Standard)
  • HY-W709413
    Panaxytriol
    Activator
    Panaxytriol is an active component of ginseng. Panaxytriol inhibits the nuclear translocation of NF-κB, thereby reducing the production of pro-inflammatory factors (such as TNF-α, IL-1β, IL-6) and nitric oxide (NO) induced by LPS (HY-D1056). Panaxytriol upregulates CYP3A4 by activating the nuclear receptor PXR/CAR. Panaxytriol improves motor dysfunction in a mouse model of brain inflammation. Panaxytriol can be used in the research of neurodegenerative diseases (such as Alzheimer's disease).
    Panaxytriol
  • HY-116568S
    Prothioconazole-d4
    Prothioconazole-d4 (JAU-6476-d4) is the deuterium labeled Prothioconazole (HY-116568). Prothioconazole is a triazolinthione fungicide. Prothioconazole is a CYP51 inhibitor.
    Prothioconazole-d<sub>4</sub>
  • HY-181611
    Polθ-IN-10
    Inhibitor
    Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers.
    Polθ-IN-10
  • HY-N4205R
    Tetrahydropiperine (Standard)
    Inhibitor
    Tetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine. This product is intended for research and analytical applications. 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).
    Tetrahydropiperine (Standard)
  • HY-B0885S
    Econazole-d6
    Econazole-d6 ((±)-Econazol-d6) is the deuterium labeled Econazole (HY-B0885). Econazole is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage.
    Econazole-d<sub>6</sub>
  • HY-W739700
    (R)-(+)-Aminoglutethimide L-Tartrate
    Inhibitor
    (R)-(+)-Aminoglutethimide (L-Tartrate) is an inhibitor of aromatase. (R)-(+)-Aminoglutethimide inhibits androstenedione with a Ki value of 0.3 μM.
    (R)-(+)-Aminoglutethimide L-Tartrate
  • HY-B1717
    Oxolamine
    Inhibitor
    Oxolamine (SKF-9976) is an orally active antitussive. Oxolamine can inhibit CYP2B1/2. Oxolamine has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine can be used in respiratory disease research.
    Oxolamine
  • HY-137931
    Testololactone
    Inhibitor
    Testololactone is an aromatase inhibitor. Testololactone can be used for research of breast carcinoma.
    Testololactone
  • HY-168210
    Antifungal agent 122
    Inhibitor
    Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-T enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity.
    Antifungal agent 122
  • HY-D0092
    7-Ethoxy-4-methylcoumarin
    99.44%
    7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6.
    7-Ethoxy-4-methylcoumarin
  • HY-145786S
    Abiraterone decanoate-d17
    Inhibitor
    Abiraterone decanoate-d17 is the deuterium labeled Abiraterone decanoate (HY-145786). Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.
    Abiraterone decanoate-d<sub>17</sub>
  • HY-W782193
    Sulcatone-d5
    Sulcatone-d5 (6-Methyl-5-hepten-2-one-d5) is the deuterium labeled Sulcatone (HY-W010435). Sulcatone (6-Methyl-5-hepten-2-one) is a plant-derived volatile organic compound with activities such as insecticidal, antifungal, and blood pressure-lowering effects. Sulcatone also serves as an insect pheromone and an endogenous metabolite, which can be found in feces. Changes in Sulcatone levels can be used for the auxiliary diagnosis of ulcerative colitis.
    Sulcatone-d<sub>5</sub>
  • HY-172808
    BNS808
    Inhibitor
    BNS808 is an orally active and selective cannabinoid-1 receptor (CB1R) antagonist (IC50 = 0.8 nM) with notable CB2R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.
    BNS808
  • HY-N2194R
    Bergamottin (Standard)
    Inhibitor
    Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
    Bergamottin (Standard)
  • HY-111906
    SCYX-6759
    Inhibitor
    SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively.
    SCYX-6759
  • HY-175195
    Adenosine receptor antagonist 6
    Inhibitor
    Adenosine receptor antagonist 6 is an orally active and selective A2A adenosine receptor (A2AAR) antagonist, with a Ki of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC50 = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.
    Adenosine receptor antagonist 6
  • HY-105408A
    Fandosentan potassium
    Inhibitor
    Fandosentan potassium is a potent endothelin A receptor (ETAR) antagonist. Fandosentan potassium inhibits CYP2C9 and CYP3A4 activities with IC50 values of 39.6 and 21.6 μM, respectively. Fandosentan potassium reverses the hypoxic pulmonary vasoconstriction in the perinatal lamb. Fandosentan potassium can be used for pulmonary hypertension research[1][2].
    Fandosentan potassium
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