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抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T63337 CYP2C19-IN-1

CYP2C19-IN-1 是强效的,无遗传毒性的、无肝脏毒性的 CYP2C19 抑制剂。 CYP2C19-IN-1 能够抑制 RNA 依赖的 RNA 聚合酶 (RdRP) (Ki: 6.16 μM),能够用于研究寨卡病毒 (ZIKV) 感染。
T63496 CYP2C9/CYP2C19-IN-1

CYP2C9/CYP2C19-IN-1 是无肝脏毒性和遗传毒性的CYP2C9/CYP2C19强效抑制剂,能够用于研究寨卡病毒 (ZIKV) 感染。
T4567 Sulfaphenazole

Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide

P450; Antibacterial Metabolism; Microbiology/Virology
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂,抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应,增加 AP-1的氧化应激和激活。
T14051 5-Hydroxylansoprazole

AG1908

Proton pump Membrane transporter/Ion channel
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole, a gastric proton-pump inhibitor that effectively treats various peptic diseases[1][2]. The metabolism of Lansoprazole occurs through CYP2C19, resulting in the formation of 5-Hydroxylansoprazole.
T78925 HIV-1 inhibitor-58

HIV-1inhibitor-58(Compound 10c)是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂,有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株,如K103N和E138K(EC50 < 50 nM)。此外,HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用(IC50分别为2.06 μM与1.91 μM),适用于HIV感染研究。
T35718 N-desmethyl Rosuvastatin (sodium salt hydrate)

N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tand...
T78590 Dibenzylfluorescein

DBF

Dibenzylfluorescein(DBF)是一款荧光探针,作为细胞色素P450(CYP)亚型,包括CYP3A4、CYP2C8、CYP2C9、CYP2C19CYP19的特异性底物,常在Km值0.87-1.9 µM(Ex=485nm,Em=535nm)范围内应用。该探针主要用于监测药物或疾病导致的CYP催化活性变化。
T79568 NPD-2975

Parasite Microbiology/Virology
NPD-2975(化合物30)是一款口服活性的抗锥虫药物,用于治疗非洲人类锥虫病(HAT)。在MRC-5人肺成纤维细胞及T. b. brucei感染的小鼠模型中,NPD-2975毒性低。此化合物展现了良好的代谢稳定性,在体外对T. b. brucei IC500抑制浓度为70 nM。NPD-2975还可抑制CYP450酶,对CYP1A2和CYP2C19的IC50分别为0.16 μM和0.42 μM。
T38131 (E)-10-Hydroxynortriptyline

(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline . Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression[1]. [1]. Shimoda K, et al. The impact of CYP2C19 and CYP2D6 genotypes on metabolism of amitriptyline in Japanese psychiatric patients. J Clin Psychopharmacol. 2002 Aug;22(4):371-8. [2]. Shimoda K, et al. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. Biotechnology ...
T62452 HIV-1 inhibitor-40

HIV-1 inhibitor-40 (Compound 4ab) 是一种 HIV-1 非核苷型逆转录酶抑制剂 (NNRTI) (EC50: 1.9 nM),体内没有明显急性毒性。HIV-1 inhibitor-40 对 CYP 的敏感性较低,作用于 CYP2C9 (IC50: 5.16 μM) 和 CYP2C19 (IC50: 4.51 μM)。
T35829 CC-90005

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...

化合物

CYP2C19-IN-1
Cat.No: T63337
Synonym:
Target:
CYP2C9/CYP2C19-IN-1
Cat.No: T63496
Synonym:
Target:
Sulfaphenazole
Cat.No: T4567
Synonym: Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide
Target: P450, Antibacterial
5-Hydroxylansoprazole
Cat.No: T14051
Synonym: AG1908
Target: Proton pump
HIV-1 inhibitor-58
Cat.No: T78925
Synonym:
Target:
N-desmethyl Rosuvastatin (sodium salt hydrate)
Cat.No: T35718
Synonym:
Target:
Dibenzylfluorescein
Cat.No: T78590
Synonym: DBF
Target:
NPD-2975
Cat.No: T79568
Synonym:
Target: Parasite
(E)-10-Hydroxynortriptyline
Cat.No: T38131
Synonym:
Target:
HIV-1 inhibitor-40
Cat.No: T62452
Synonym:
Target:
CC-90005
Cat.No: T35829
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S2360 Corydaline

Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline

P450; Virus Protease; Opioid Receptor; AChE Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。

天然产物

Corydaline
Cat.No: T5S2360
Synonym: Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline
Target: P450, Virus Protease, Opioid Receptor, AChE
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