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

Cytochrome P450

CYPs

Cytochrome P450

Related Products

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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.

Cytochrome P450 Isoform Specific Products:

Cytochrome P450 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114955
    MTTC
    MTTC is a 1,2,3-thiadiazole compound that exhibits mechanism-based inactivation, resulting in the inactivation of cytochrome P450 2E1 activity.
    MTTC
  • HY-B0822S1
    Fipronil-13C6
    		Activator
    Fipronil-13C6 is the 13C-labeled Fipronil. 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 (IC50s = 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.
    Fipronil-<sup>13</sup>C<sub>6</sub>
  • HY-173033
    MI-883
    		Modulator
    MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models.
    MI-883
  • HY-W010435R
    Sulcatone (Standard)
    		Inhibitor
    Sulcatone (Standard) (6-Methyl-5-hepten-2-one (Standard)) is the analytical standard of Sulcatone (HY-W010435). This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0370S
    Bergapten-d3
    		Inhibitor
    Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten-d<sub>3</sub>
  • HY-17356G
    Fenofibrate (GMP)
    		Inhibitor
    Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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.
    Fenofibrate (GMP)
  • HY-121500
    R-116010
    		Inhibitor
    R-116010 is a potent and selective retinoic acid (RA) metabolism inhibitor and can inhibit hydroxylase CYP26. R-116010 can enhance the anti-tumor effect of retinoic acid drugs. R-116010 can be used for the research of cancer, metabolic and neurological disease, such as neuroblastoma.
    R-116010
  • HY-121789S
    Proadifen-d2
    		Inhibitor
    Proadifen-d2 is the deuterium labeled Proadifen (HY-121789).
    Proadifen-d<sub>2</sub>
  • HY-N7781R
    (-)-(E)-Guggulsterone (Standard)
    		Inhibitor
    (-)-(E) -guggulsterone (Standard) is the analytical standard for (-)-(E) -guggulsterone ((E)-Guggulsterone) (HY-N7781). (-)-(E)-Guggulsterone is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone (Standard)
  • HY-122410S
    Dihydrolanosterol-d7
    		99.0%
    Dihydrolanosterol-d7 is deuterium labeled Dihydrolanosterol. Dihydrolanosterol is a subtrate of CYP51 and a cholesterol biosynthesis inhibitor.
    Dihydrolanosterol-d<sub>7</sub>
  • HY-175554
    CYP1B1-IN-10
    		Inhibitor
    CYP1B1-IN-10 (Compound 15C) is a highly selective human cytochrome P450 1B1 (hCYP1B1) inhibitor (IC50=0.11 μM). CYP1B1-IN-10 is promising for research of hormone-dependent tumors (e.g., breast and ovarian cancers).
    CYP1B1-IN-10
  • HY-119293A
    K777 tosylate
    		Inhibitor
    K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively.
    K777 tosylate
  • HY-178479
    IDO1-IN-30
    		Activator
    IDO1-IN-30 (Compound (R)-100) is a potent and highly selective IDO1 inhibitor. IDO1-IN-30 has an IC50 of 4.8 nM to IDO1 in SKOV3 cells. IDO1-IN-30 does not show significant cytotoxicity at 25 µM in HepG2 cells. IDO1-IN-30 can eliminate inhibition of CYP450 enzymes (such as 3A4, 2C9, 2D6). IDO1-IN-30 can be used for research on cancer and inflammatory conditions.
    IDO1-IN-30
  • HY-N2181A
    DL-Acetylshikonin
    		Inhibitor
    DL-Acetylshikonin is a non-selective, reversible cytochrome P450 inhibitor with IC50 values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities.
    DL-Acetylshikonin
  • HY-167872
    Bifeprofen
    		Inhibitor
    Bifeprofen, a cytochrome P450 2C9 (CYP2C9) inhibitor, exhibits dose-dependent inhibition (75 μM, 50%).
    Bifeprofen
  • HY-10779
    BMS-344577
    		Inhibitor
    BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC50 = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC50 = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease.
    BMS-344577
  • HY-14863
    Lunacalcipol
    		Antagonist
    Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT).
    Lunacalcipol
  • HY-113739A
    (S)-Desmethylcitalopram
    		Inhibitor
    (S)-Desmethylcitalopram is the isomer of Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6，-2C19 with IC50s of 39.5 and 53.5 μM.
    (S)-Desmethylcitalopram
  • HY-118216
    Bitertanol
    		Modulator 98.70%
    Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an CYP1A1, CYP2B, and CYP3A inducer in vivo and an CYP1A inhibitor in vitro.
    Bitertanol
  • HY-156330
    HIV-IN-9
    HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6.
    HIV-IN-9
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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