1. シグナル伝達
  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.

製品番号 製品名 製品効果 純度 構造式
  • HY-121872
    DP-b99 Inhibitor
    DP-b99 is a blood-brain barrier-permeable inhibitor of CYP2C9 and MMP-9, with a Ki value of 4.655 μM against CYP2C9. DP-b99 inhibits CYP2C9 via apparent non-competitive inhibition, mainly chelates pathological Zn2+ in the membrane environment, attenuates the elevation of intracellular Zn2+ and Ca2+ levels, delays seizure onset and reduces seizure severity, and also prevents MMP-9-dependent dendritic spine remodeling, β-dystroglycan cleavage and gelatinase activity. DP-b99 can be used in the research of acute ischemic stroke, epileptogenesis and stroke.
    DP-b99
  • HY-B1218R
    Sulfaphenazole (Standard) Inhibitor
    Sulfaphenazole (Standard) is the analytical standard of Sulfaphenazole. This product is intended for research and analytical applications. Sulfaphenazole is a selective inhibitor of human cytochrome P450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion.
    Sulfaphenazole (Standard)
  • HY-B0113R
    Omeprazole (Standard)
    Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. Omeprazole (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.
    Omeprazole (Standard)
  • HY-132845
    Utreloxastat Inhibitor 99.32%
    Utreloxastat (PTC857) is an orally active and blood-brain barrier-permeable 15-lipooxygenase inhibitor. Utreloxastat is a weak inhibitor of CYP1A2 and 2B6 with an IC50 of >5.3 μM. Utreloxastat reduces oxidative stress and inhibits the consumption of reduced glutathione and ferroptosis. Utreloxastat can be used in the study of neurodegenerative diseases characterized by high levels of oxidative stress and mitochondrial pathology, such as amyotrophic lateral sclerosisc.
    Utreloxastat
  • HY-111430
    1-Ethynylnaphthalene

    1-Ethynylnaphthalene

    Inhibitor 99.27%
    1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. 1-Ethynylnaphthalene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    1-Ethynylnaphthalene
  • HY-A0296
    Chlormethiazole hydrochloride

    Chlormethiazole hydrochloride

    Inhibitor 99.94%
    Clomethiazole hydrochloride is a potent and orally active GABAA agonist. Clomethiazole hydrochloride inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Clomethiazole hydrochloride is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
    Chlormethiazole hydrochloride
  • HY-A0064R
    Verapamil hydrochloride (Standard) Inhibitor
    Verapamil (hydrochloride) (Standard) is the analytical standard of Verapamil (hydrochloride). This product is intended for research and analytical applications. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
    Verapamil hydrochloride (Standard)
  • HY-17570
    Desoximetasone

    Desoximetasone

    Substrate 98.72%
    Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis.
    Desoximetasone
  • HY-117147A
    GSK2945 hydrochloride Activator 98.49%
    GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
    GSK2945 hydrochloride
  • HY-17508S1
    Clarithromycin-d3 Inhibitor 99.90%
    Clarithromycin-d3 is the deuterium labeled Clarithromycin (HY-17508). Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Clarithromycin-d<sub>3</sub>
  • HY-N0153R
    Naringin (Standard) Inhibitor
    Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1).
    Naringin (Standard)
  • HY-152118
    CYP1B1-IN-4 Inhibitor 99.09%
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes.
    CYP1B1-IN-4
  • HY-129923
    (R)-Omeprazole sodium Inhibitor 98.07%
    (R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19.
    (R)-Omeprazole sodium
  • HY-B0589C
    (3S,5S)-Atorvastatin Activator
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
    (3S,5S)-Atorvastatin
  • HY-N0292R
    Oleuropein (Standard) Inhibitor
    Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
    Oleuropein (Standard)
  • HY-B0852R
    Tebuconazole (Standard) Inhibitor
    Tebuconazole (Standard) is the analytical standard of Tebuconazole. This product is intended for research and analytical applications. Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
    Tebuconazole (Standard)
  • HY-121188
    DDMS Inhibitor 99.19%
    DDMS (Dibromo-dodecenyl-methylsulfimide) is a selective 20-HETE production inhibitor. DDMS attenuates the vasodilatory response to sodium nitroprusside (SNP).
    DDMS
  • HY-B1880
    Oxadiazon

    オキサジアゾン

    Inhibitor 98.51%
    Oxadiazon is an orally active herbicide. Oxadiazon reduces hepatic cytochrome P450 levels. Oxadiazon increases palmitoyl CoA oxidase, acetyl carnitine transferase, and hepatic ALAS activity. Oxadiazon induces hepatomegaly and experimental porphyria. Oxadiazon controls weeds. Oxadiazon may be used in neurodegenerative disease research.
    Oxadiazon
  • HY-171459
    LEQ803 99.37%
    LEQ803 (N-Desmethyl Ribociclib) is a drug metabolite of the CDK4/6 inhibitor Ribociclib (HY-15777), which is produced through metabolism by CYP3A4. LEQ803 has potential application value in the field of oncology.
    LEQ803
  • HY-B0973
    Dibenzothiophene Inhibitor 99.92%
    Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a Km of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms.
    Dibenzothiophene
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