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

Cytochrome P450 (细胞色素P450)

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 相关产品 (113):

Cat. No. Product Name Effect Purity
  • HY-A0064
    Verapamil hydrochloride Inhibitor 99.95%
    Verapamil hydrochloride ((±)-Verapamil hydrochloride) 是一种钙通道 (calcium channel) 阻滞剂,是一种有效的口服活性的第一代 P 糖蛋白 (P-gp) 抑制剂。Verapamil hydrochloride 能也抑制 CYP3A4,并可用于高血压,心律不齐和心绞痛的研究。
  • HY-N1201
    Apigenin Inhibitor 99.22%
    Apigenin (4',5,7-Trihydroxyflavone) 是一种竞争性 CYP2C9 抑制剂,Ki 为 2 μM。
  • HY-17356
    Fenofibrate Inhibitor 99.92%
    Fenofibrate 是一种选择性的 PPARα 激动剂,EC50 为 30 μM。Fenofibrate 抑制细胞色素 P450 亚型, 对 CYP2C19CYP2B6CYP2C9CYP2C8CYP3A4IC50 分别为 0.2,0.7,9.7,4.8 和 142.1 μM。
  • HY-75054
    Abiraterone acetate Inhibitor 99.97%
    Abiraterone acetate (CB7630) 是一种口服、有效、选择性和不可逆的 CYP17A1 抑制剂,具有抗雄激素活性。Abiraterone acetate是 Abiraterone (CB7598) 的前药形式。
  • HY-17514
    Itraconazole Inhibitor 99.15%
    Itraconazole (R51211) 是一种三唑类抗真菌药,也是一种有效的口服活性的 Hedgehog 信号通路拮抗剂,IC50 约为 800 nM。Itraconazole 可有效抑制羊毛甾醇 14α-脱甲基酶 (Cytochrome P450) ,从而抑制羊毛甾醇向麦角固醇的氧化转化。Itraconazole 具有抗癌和抗血管生成作用。
  • HY-N0692
    Schisandrol B Inhibitor 99.57%
    Schisandrol B (Gomisin-A) 是 Schisandra sphenanthera 的主要活性成分,具有保肝作用。Schisandrol B 抑制活性氧 (ROS) 的产生。Schisandrol B 抑制 P-糖蛋白和 CYP3A 的活性,还具有抗炎,抗糖尿病和抗氧化的作用。
  • HY-N8094
    Kushenol M Inhibitor
    Kushenol M 是一种黄酮类化合物,在 Sophora flavescens 发现。 Kushenol M 是一种细胞色素 P450 (CYP) 抑制剂,对人肝微粒体中 CYP3A4 抑制作用的 IC50 值为 1.29 μM。
  • HY-131452
    1-Ethynylpyrene Inhibitor
    1-Ethynylpyrene 是细胞色素 P450 1A1, 1A22B1 的抑制剂,IC50 分别为 0.18,0.32 和 0.04 μM。
  • HY-103389
    1-Aminobenzotriazole Inhibitor 99.88%
    1-Aminobenzotriazole 是细胞色素 P450 (P450) 的非特异且不可逆抑制剂。
  • HY-B0105
    Ketoconazole Inhibitor 99.47%
    Ketoconazole (R-41400) 是咪唑类抗真菌剂,是经典的CYP3A4抑制剂,也是 CYP24A1的抑制剂。
  • HY-70013
    Abiraterone Inhibitor 99.61%
    Abiraterone 是一种有效的不可逆的 CYP17A1 抑制剂,具有抗雄激素活性,抑制细胞色素 p450 酶 CYP17 的 17α-羟化酶和 17,20-裂合酶活性,IC50 值 分别为 2.5 nM 和 15 nM.
  • HY-14531
    Talarozole Inhibitor 99.78%
    Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂 (RAMBA),可提高内源性全反式维甲酸 (RA) 的细胞内水平。Talarozole 抑制 CYP26A1CYP26B1IC50 值分别为 5.4 和 0.46 nM。
  • HY-17367A
    Atazanavir sulfate Inhibitor 99.94%
    Atazanavir sulfate (BMS-232632 sulfate) 是一种高选择性的 HIV-1蛋白酶抑制剂,用于艾滋病毒感染的研究。Atazanavir sulfate (BMS-232632 sulfate) 是 CYP3A4 的底物和抑制剂,也是 P-糖蛋白的抑制剂和诱导剂。
  • HY-17508
    Clarithromycin Inhibitor >98.0%
    Clarithromycin是大环内脂类抗生素,还是CYP3A4抑制剂。
  • HY-B0365A
    Memantine hydrochloride Inhibitor >98.0%
    Memantine (hydrochloride) (D-145 (hydrochloride)) 是金刚胺衍生物,是一种温和的 NMDA 受体 (NMDA receptor) 非竞争性拮抗剂, 能够抑制 CYP2B6 和 CYP2D6。
  • HY-13832
    Atovaquone Inhibitor 99.81%
    Atovaquone (Atavaquone) 是一种有效的、具有口服活性的选择性寄生虫线粒体细胞色素 bc1 (parasite’s mitochondrial cytochrome bc1) 复合物的抑制剂。Atovaquone 抑制人类和 P. falciparum 细胞色素 bc1 活性,IC50 值分别为 460 nM 和 2.0 nM。Atovaquone 是一种抗疟 (antimalarial agent) 试剂,有潜力用于肺孢子虫肺炎、弓形体病、疟疾和巴贝斯虫病的相关研究。
  • HY-B1232
    Metyrapone Inhibitor 99.84%
    Metyrapone抑制P450介导的ω/ω-1羟化酶活性和CYP11B1。
  • HY-107204
    Furafylline Inhibitor 99.86%
    Furafylline 是一种有效且有选择性的人细胞色素 P450IA2 抑制剂,其 IC50 值为 0.07 μM。
  • HY-B0258
    Gemfibrozil Inhibitor 99.91%
    Gemfibrozil 是一种 PPAR-α 激活剂,为一种降脂药;Gemfibrozil 同时是 P450 的非选择性抑制剂,对 CYP2C9,2C19,2C8 和 1A2 的 Ki 值分别为 5.8,24,69 和 82 μM。
  • HY-N0382
    Galangin Inhibitor 99.96%
    Galangin (Norizalpinin) 是 arylhydrocarbon 受体的调节剂,同时抑制 CYP1A1 的活性。
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