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

Cytochrome 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 (99):

Cat. No. Product Name Effect Purity
  • HY-N1201
    Apigenin Inhibitor >98.0%
    Apigenin 是一种竞争性 CYP2C9 抑制剂,Ki 为 2 μM。
  • HY-75054
    Abiraterone acetate Inhibitor 99.97%
    Abiraterone acetate 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-17356
    Fenofibrate Inhibitor 99.92%
    Fenofibrate是 PPARα 激动剂,EC50 为30 μM。
  • HY-14531
    Talarozole Inhibitor 99.54%
    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-10493
    Cobicistat Inhibitor 99.77%
    Cobicistat是有效,选择性的细胞色素酶P450 3A (CYP3A)抑制剂,IC50为30-285 nM。 Cobicistat是一种药代动力学增强剂,可增强治疗HIV药物的吸收。
  • HY-N0482
    Phillyrin Activator 98.99%
    Phillyrin 是从连翘中分离出来的,具有抗菌和消炎作用。Phillyrin 对大鼠 CYP1A2CYP2D1 具有潜在的诱导作用,而不会影响 CYP2C11 和 CYP3A1/2 活性。
  • HY-124527
    HET0016 Inhibitor
    HET0016 是一种高效、选择性的 20-HETE 合成酶抑制剂,对重组 CYP4A1、CYP4A2 和 CYP4A3 催化 20-HETE 合成作用的 IC50 值分别为 17.7 nM, 12.1 nM 和 20.6 nM。HET0016 是一种选择性 CYP450 抑制剂,已被证明可以抑制血管生成和肿瘤生长。
  • HY-128859
    EMT inhibitor-2 Inhibitor
    EMT inhibitor-2 (Compound 1) 抑制由免疫细胞释放的物质如 IL-1β 和 TGF-β 诱导的上皮-间质转化 (EMT)。EMT inhibitor-2 抑制CYP3A4 睾酮和 CYP2C9,IC50 分别为 49.72 和 5.54 μM。
  • HY-B0105
    Ketoconazole Inhibitor 99.67%
    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-14273
    Isavuconazole Inhibitor 99.99%
    Isavuconazole (BAL-4815) 是一种三唑类前药,对酵母、霉菌和二型真菌具有抗真菌活性。Isavuconazole 抑制麦角固醇生物合成,导致真菌膜结构和功能的破坏。Isavuconazole 是 CYP3A4 的中度抑制剂。
  • 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,用于治疗艾滋病毒感染,是第一个批准每天使用一次的蛋白酶抑制剂。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-B0365A
    Memantine hydrochloride Inhibitor >98.0%
    Memantine (hydrochloride) (D-145 (hydrochloride)) 是金刚胺衍生物,对 NMDA 受体有较弱到适中的亲和力, 能够抑制CYP2B6和YP2D6。
  • 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-B1232
    Metyrapone Inhibitor 99.84%
    Metyrapone抑制P450介导的ω/ω-1羟化酶活性和CYP11B1。
  • 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-17508
    Clarithromycin Inhibitor >98.0%
    Clarithromycin是大环内脂类抗生素,还是CYP3A4抑制剂。
  • 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-N0893
    Tetrahydrocurcumin Inhibitor
    Tetrahydrocurcumin 在姜黄 (Curcuma longa) 中发现的一种姜黄素,是由 Curcumin 还原产生的。Tetrahydrocurcumin 抑制 CYP2C9CYP3A4
  • HY-N0153
    Naringin Inhibitor 99.79%
    Naringin是黄烷酮糖苷,有很多药理作用,例如抗氧化活性,降血脂,抗癌,抑制细胞色素P450酶。
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