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-A0016R
    Dronedarone (Standard)
    Inhibitor
    Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone (Standard)
  • HY-135549R
    Fluxapyroxad (Standard)
    Inhibitor
    Fluxapyroxad (Standard) is the analytical standard of Fluxapyroxad. This product is intended for research and analytical applications. Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species.
    Fluxapyroxad (Standard)
  • HY-17514R
    Itraconazole (Standard)
    Inhibitor
    Itraconazole (Standard) is the analytical standard of Itraconazole. This product is intended for research and analytical applications. 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.
    Itraconazole (Standard)
  • HY-W082430
    CYP2A6-IN-2
    Inhibitor
    CYP2A6-IN-2 (compound 5) is a CYP2A6 inhibitor. CYP2A6-IN-2 can be used in the study of nicotine dependence.
    CYP2A6-IN-2
  • HY-13632S6
    Exemestane-d4
    Inhibitor
    Exemestane-d4 (FCE 24304-d4) is deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
    Exemestane-d<sub>4</sub>
  • HY-123562
    GNF7686
    Inhibitor
    GNF7686 is a cytochrome b inhibitor. GNF7686 exhibits inhibitory activity against complex III in the extracts of L. donovani and T. cruzi.
    GNF7686
  • HY-B0876R
    Fomepizole (Standard)
    Inhibitor
    Fomepizole (Standard) is the analytical standard of Fomepizole. This product is intended for research and analytical applications. 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.
    Fomepizole (Standard)
  • HY-10493R
    Cobicistat (Standard)
    Inhibitor
    Cobicistat (Standard) is the analytical standard of Cobicistat. This product is intended for research and analytical applications. 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.
    Cobicistat (Standard)
  • HY-163804
    Cyprocide-B
    Modulator
    Cyprocide-B is activated by Cytochrome P450 and converted to electrophilic metabolites that selectively kill nematodes C. elegans. Cyprocide-B is promising for research of selective nematicide.
    Cyprocide-B
  • HY-135334S
    ACP-5862-d4
    Inhibitor
    ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
    ACP-5862-d<sub>4</sub>
  • HY-13632S2
    Exemestane-d3
    Inhibitor
    Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
    Exemestane-d<sub>3</sub>
  • HY-N0921R
    Dihydromethysticin (Standard)
    Activator
    Dihydromethysticin (Standard) is the analytical standard of Dihydromethysticin. This product is intended for research and analytical applications.
    Dihydromethysticin (Standard)
  • HY-118216R
    Bitertanol (Standard)
    Modulator
    Bitertanol (Standard) is the analytical standard of Bitertanol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-139382
    2-(Isopentylamino)naphthalene-1,4-dione
    Inhibitor
    2-(Isopentylamino)naphthalene-1,4-dione (compound 3d), a Vitamin K (HY-B2172) analogue, shows protection in Pentylenetetrazole (PTZ)-induced seizure model. 2-(Isopentylamino)naphthalene-1,4-dione significantly increases ATP levels in zebrafish as well as HT-22 cells. 2-(Isopentylamino)naphthalene-1,4-dione shows excellent permeability into the brain.
    2-(Isopentylamino)naphthalene-1,4-dione
  • HY-155456
    CYP2A6-IN-1
    Inhibitor
    CD-6 is a flavonoid CYP2A6 inhibitor (IC50: 1.566 μM). CYP2A6 inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases.
    CYP2A6-IN-1
  • HY-N0688R
    Linderane (Standard)
    Inhibitor
    Linderane (Standard) is the analytical standard of Linderane. This product is intended for research and analytical applications. Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.
    Linderane (Standard)
  • HY-W401407
    Diosmetin-3-O-glucuronide
    Diosmetin-3-O-glucuronide is a major circulating metabolite of Diosmetin (HY-N0125) in plasma and in urine. Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity.
    Diosmetin-3-O-glucuronide
  • HY-145751
    7α-Hydroxy-DHEA
    7α-Hydroxy-DHEA (7α-Hydroxydehydroepiandrosterone) is a 7α-hydroxylated metabolite of DHEA (HY-14650), catalyzed by intracellular steroid 7α-hydroxylases such as P450 2A1. 7α-Hydroxy-DHEA exhibits biological activity comparable to DHEA but does not convert into compounds with androgenic or estrogenic activity. It induces the activity of thermogenic enzymes such as mitochondrial sn-glycerol-3-phosphate dehydrogenase and cytosolic malic enzyme, enhancing heat production and reducing food utilization efficiency. As a more efficient and safer metabolite compared to DHEA, 7α-Hydroxy-DHEA holds potential for studies in the fields of obesity, metabolic diseases, and adrenal carcinoma.
    7α-Hydroxy-DHEA
  • HY-17643R
    Oteseconazole (Standard)
    Inhibitor
    Oteseconazole (Standard) is the analytical standard of Oteseconazole. This product is intended for research and analytical applications. Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (Kd ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes.
    Oteseconazole (Standard)
  • HY-170920
    Herbicide safener-4
    Activator
    Herbicide safener-4 (Compound I-15) is a Herbicide safener, improving the herbicide resistance of crops without reducing the herbicidal effect on targeted weed species. Herbicide safener-4 competitively binds to the ALS active site with Mesosulfuron-methyl (HY-126987). Herbicide safener-4 enhances GSH (HY-D0187), GST, CYP450, POD, SOD and ALS activity in plants.
    Herbicide safener-4
Cat. No. Product Name / Synonyms Application Reactivity

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