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P450

Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.

Products for  P450

  1. Cat.No. 产品名称 Information
  2. GC91296 p-Carboxyphenyl Sulfate

    一种硫酸化的酚酸。

  3. GC91226 10-Chloroestra-1,4-diene-3,17-dione

    一种雌激素受体α激动剂

  4. GC91189 Piperonyl Butoxide-d9

    一种用于定量苯甲酸对氧乙基的内部标准。

  5. GC91128 Imazalil-d5 (sulfate)

    一种用于量化伊马唑啉的内部标准

  6. GC90195 Posaconazole-d5

    一种用于量化泊沙康唑的内部标准。

  7. GC69602 Obtusifoliol Obtusifoliol 是一种特异的 CYP51 抑制剂,Obtusifoliol 对布鲁氏锥虫 (TB) 和人 CYP51 的亲和力的 Kd 值分别为 1.2 µM 和 1.4 µM。
  8. GC68926 TP0472993 CYP4A11/CYP4F2-IN-2 是一种有效和具有口服活性的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双抑制剂,IC50 值分别分别为 140 nM 和 40 nM。CYP4A11/CYP4F2-IN-2 具有研究肾脏疾病的潜力。
  9. GC68863 Cholesterol 24-hydroxylase-IN-1 Cholesterol 24-hydroxylase-IN-1 (compound 17) 是一种强效、口服活性和高选择性的胆固醇24-羟化酶 (CH24H or CYP46A1) 抑制剂 (IC50=8.5 nM)。Cholesterol 24-hydroxylase-IN-1 能透过血脑屏障。
  10. GC68544 4,5-Dimethoxycanthin-6-one 4,5-Dimethoxycanthin-6-one 是一种有效的、非竞争性的 CYP1A2 介导的 phenacetin O-deethylation 抑制剂,其 IC50 值为 1.7 μM, Ki 值为 2.6 μM。4,5-Dimethoxycanthin-6-one 为生物碱,从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到。
  11. GC67933 LKY-047 LKY-047,是 Decursin 的一种衍生物,是一种有效的选择性的可逆竞争性的细胞色素 P45022J2 (CYP2J2) 抑制剂,IC50 为 1.7 μM。LKY-047 对其他人类 P450 无效,例如 CYP1A2、CYP2A6、CYP2B6、CYP2C8、CYP2C9、CYP2C19、CYP2D6、CYP2E1 和 CYP3A。
  12. GC66197 α-?Terpinyl acetate Terpinyl Acetate (alpha-Terpinyl), a naturally occuring compound found in several essential oils, is a flavouring agent.
  13. GC52132 N-desmethyl Diltiazem (hydrochloride) An active metabolite of diltiazem
  14. GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone 是大鼠肝细胞色素 P450 酶的荧光探针底物。
  15. GC65345 BI 653048 BI 653048 是一种选择性且口服的非甾体类糖皮质激素 (glucocorticoid (GC)) 激动剂,其 IC50 值为 55 nM。BI 653048 抑制 CP1A2,CYP2D6,CYP2C9,CYP2C19 和 CYP3A4 的活性并降低对 hERG 离子通道的亲和力 (IC50>30 μM)。BI 653048 源于专利 WO2005028501A1 (化合物 103),它也是一种 HCV NS3 protease 抑制剂,可以减少感染丙型肝炎病毒的病毒载量。
  16. GC65260 EDP-305 EDP-305 是一种口服有效且选择性的 farnesoid X 受体 (FXR) 激动剂,其 EC50 值为 34 nM (CHO 细胞嵌合性 FXR) 和 8 nM (HEK 细胞全长 FXR)。EDP-305 显示出强大而持久的抗纤维化作用。EDP-305 可用于原发性胆道胆管炎 (PBC) 和非酒精性脂肪性肝炎 (NASH) 研究。
  17. GC65088 Atovaquone-d5 Atovaquone-d5 (Atavaquone-d5) 是 Atovaquone 的氘代物。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。
  18. GC52083 21-Deoxycortisone A corticosteroid metabolite of 11-keto progesterone
  19. GC52062 7-Benzyloxy-4-(trifluoromethyl)coumarin A fluorogenic substrate for CYP1A2 and CYP3A
  20. GC52060 Trimipramine N-oxide An active metabolite of trimipramine
  21. GC52045 N-desmethyl Azelastine An active metabolite of azelastine
  22. GC52038 Desthiazolylmethyl Ritonavir A ritonavir degradation product
  23. GC52024 Aripiprazole N-oxide A metabolite of aripiprazole
  24. GC52019 Norpropranolol (hydrochloride) An active metabolite of propranolol
  25. GC52007 N-hydroxylamine Dapsone An active metabolite of dapsone
  26. GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine
  27. GC49866 Desmethyl Carvedilol An active metabolite of carvedilol
  28. GC49855 Harmalol (hydrochloride hydrate) A β-carboline alkaloid and an active metabolite of harmaline
  29. GC49851 Norquetiapine An active metabolite of quetiapine
  30. GC49842 Digoxigenin Bisdigitoxoside A Na+/K+-ATPase inhibitor
  31. GC49832 Hydroxymetronidazole An active metabolite of metronidazole
  32. GC49817 Desethoxy Quetiapine (hydrochloride) An active metabolite of quetiapine
  33. GC64010 Abiraterone decanoate Abiraterone decanoate 是一种有效的 Abiraterone 前药。Abiraterone decanoate 通过肌肉内 (IM) 递送提供 Abiraterone 的受控释放和长效 CYP17 抑制。
  34. GC63872 Dagrocorat hydrochloride Dagrocorat (PF-00251802) hydrochloride 是一种具有口服活性,选择性和高亲和性部分糖皮质激素受体的激动剂。Dagrocorat hydrochloride 也是一种时间依赖性可逆抑制剂,对 CYP3A (IC50=1.3 μM) 和CYP2D6 (Ki=0.57 μM) 有抑制作用。Dagrocorat hydrochloride 可用于类风湿性关节炎的研究。
  35. GC49686 N-desmethyl Regorafenib N-oxide An active metabolite of regorafenib
  36. GC49629 6β-hydroxy Prednisolone A metabolite of prednisolone
  37. GC49627 Rabeprazole sulfone A metabolite of rabeprazole
  38. GC49583 N-desmethyl Sertraline (hydrochloride) A metabolite of sertraline
  39. GC49559 Hydroxymethyl Tolperisone (hydrochloride) A metabolite of tolperisone
  40. GC49544 8-hydroxy Mirtazapine A metabolite of mirtazapine
  41. GC49503 Thujopsene A sesquiterpene with diverse biological activities
  42. GC49501 Nirvanol An active metabolite of mephenytoin
  43. GC63469 Abiraterone-D4 Abiraterone-D4 (CB-7598-D4) 是 Abiraterone 的氘代物。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.
  44. GC63272 β-Apo-8’-carotenal Apocarotenal is a carotenoid found in spinach and citrus fruits and plays a role as a precursor of vitamin A.
  45. GC63199 Soticlestat A cholesterol 24-hydroxylase/CYP46A1 inhibitor
  46. GC49439 (±)11(12)-DiHET MaxSpec® Standard A quantitative analytical standard guaranteed to meet MaxSpec® identity, purity, stability, and concentration specifications
  47. GC49429 6-keto Lithocholic Acid A metabolite of lithocholic acid
  48. GC49421 Atorvastatin lactone-d5 An internal standard for the quantification of atorvastatin lactone
  49. GC49410 CVT-2738 An active metabolite of ranolazine
  50. GC49409 Desmethyl Ranolazine A metabolite of ranolazine
  51. GC49403 Benzarone An active metabolite of benzbromarone

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