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Search Results for " cyp3a "

25

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T22437	Tazofelone LY-213829	Others	Others
	Tazofelone (LY-213829) 是环氧合酶-II (COX-II) 抑制剂。在 CYP3A 介导下，Tazofelone 可转化为亚砜和喹啉代谢物，可用于研究炎症性肠病。
T7788	2-Phenyl-2-(1-piperidinyl)propane	Others	Others
	2-Phenyl-2-(1-piperidinyl)propane 是一种具有可逆性、选择性的人 CYP2B6抑制剂，其 IC50为 5.1 μM，Ki 为 5.6。它对 CYP2D6 、CYP3A 均有抑制作用，且 IC50值分别为74 μM、200 μM。
T6246	Cobicistat Tybost,GS-9350,考西司他	P450; HIV Protease	Metabolism; Microbiology/Virology; Proteases/Proteasome
	Cobicistat (GS-9350) 是一种细胞色素酶P450 3A 的选择性抑制剂，IC50值为30-285 nM。它是一种药代动力学增强剂，可增强抗 HIV 药物的吸收。
T77698	hCYP3A4 Fluorogenic substrate 1	Others	Others
	hCYP3A4 Fluorogenic substrate 1 是邻苯二甲酰亚胺衍生物，对 COX 表现出低活性。
T79343	hCYP3A4-IN-1
	hCYP3A4-IN-1（化合物C6）是一种经口服时具有活性的hCYP3A4抑制剂，其对hCYP3A4的IC50值在人肝微粒体(HLM)为43.93 nM，在CHO-3A4稳定转染细胞系中为153.00 nM。hCYP3A4-IN-1通过竞争性抑制机制，有效抑制CYP3A4催化的N-乙基-1,8-萘二甲酰亚胺(NEN)羟基化反应，其Ki值为30.00 nM。
T63954	CYP3A4-IN-1
	CYP3A4-IN-1 是细胞色素 P450 3A4 (CYP3A4) 的有效抑制剂 (IC50: 0.085 μM)。
T64032	CYP3A4-IN-3
	CYP3A4-IN-3 是特异性的、高度亲和力的细胞色素 P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) 抑制剂 (IC50: 0.075 μM)。CYP3A4-IN-3 是利托那韦类似物，结构更加简单，且抑制效果是利托那韦的两倍。CYP3A4-IN-3 能够用做抗病毒剂和免疫抑制剂。
T64037	CYP3A4-IN-2
	CYP3A4-IN-2 是细胞色素 P450 3A4 (CYP3A4) (cytochrome P450 3A4 (CYP3A4)) 的特异性抑制剂 (IC50: 0.055 μM)。CYP3A4-IN-2 是利托那韦类似物，与利托那韦相比，其 R2 侧基的疏水性更高，抑制作用更强。CYP3A4-IN-2 能够作为免疫抑制剂及抗病毒剂。
T13600	CDD3505 4-nitro-1-trityl-1H-imidazole	P450	Metabolism
	CDD3505 (4-nitro-1-trityl-1H-imidazole) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。
T13601	CDD3506 1-TRITYL-1H-IMIDAZOL-4-AMINE	P450	Metabolism
	CDD3506 (1-TRITYL-1H-IMIDAZOL-4-AMINE) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。
T21818	Pregnenolone Carbonitrile Pregnenolone 16α-carbonitrile ,5-Pregnen-3β-ol-20-one-16α-carbonitrile	P450	Metabolism
	Pregnenolone Carbonitrile (5-Pregnen-3β-ol-20-one-16α-carbonitrile) 是一种啮齿动物-PXR 的激活剂，可诱导 CYP3A 的表达。
T22025	AG 045572	P450; GNRH Receptor	GPCR/G Protein; Metabolism
	AG 045572 是一种有效的 GnRH 受体拮抗剂，对人类和大鼠的 GnRH receptor 具有抑制作用， Ki 值分别为 6.0 nM 和 3.8 nM。AG 045572 通过 CYP3A 代谢并抑制睾酮。
T0120	Voriconazole UK-109496,伏立康唑	Antifection; Antifungal	Microbiology/Virology
	Voriconazole (UK-109496) 是一种三唑类抗真菌剂，可抑制真菌麦角甾醇的生物合成。它特异性抑制由真菌细胞色素 P450 酶介导的 14-α-羊毛甾醇去甲基化作用
T8339	16α-Hydroxyprednisolone 16alpha-羟基泼尼松龙,16alpha-Hydroxyprednisolone	Others; Drug Metabolite	Metabolism; Others
	16α-Hydroxyprednisolone 是糖皮质激素布地奈德 22(R) epimer 构型的代谢物，经过 CYP3A 酶代谢生成。
T21548	PF-4981517 CYP3cide	P450	Metabolism
	PF-4981517 (CYP3cide) 是一种高效，特异性和时间依赖性细胞色素P4503A4 (CYP3A4)抑制剂。对于CYP3A4，CYP3A5 和 CYP3A7，抑制CYP3A 活性的IC50值分别为 0.03 μM，17 μM 和 71μM。PF-4981517 可用于区分CYP3A4和 CYP3A5 对于药物代谢的作用。
T28400	Phenoprolamine Hydrochloride phenoprolamine,DDPH
	Phenoprolamine Hydrochloride is an adrenergic α1 receptor antagonist with potent antihypertensive, neuroprotective and cardioprotective effects. Phenoprolamine Hydrochloride inhibits CYP2D and CYP3A activities and down-regulates their mRNA transcription a
T36429	Dihydrodiol-Ibrutinib
	PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)
T36723	Desmethyl Ranolazine
	Desmethyl ranolazine is a metabolite of the antianginal agent ranolazine .1It is formed from ranolazine by the cytochrome P450 (CYP) isoform CYP3A. 1.Wang, Y., Chen, X., Sun, Z., et al.Development and validation of a sensitive LC-MS/MS assay for simultaneous quantitation of ranolazine and its three metabolites in human plasmaJ. Chromatogr. B889-89010-16(2012)
T11002	Desethylamiodarone hydrochloride N-desethylamiodarone hydrochloride,LB 33020 hydrochloride	Others	Others
	Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is formed by the CYP3A isozyme. Amiodarone is an antiarrhythmic drug that inhibits ATP-sensitive potassium channels with an IC50 of 19.1 μM. It is the main active metabolite of amiodaro
T71302	Norfluoxetine-d5 HCl
	Norfluoxetine-d5 is intended for use as an internal standard for the quantification of norfluoxetine by GC- or LC-MS. Norfluoxetine is an active metabolite of the antidepressant fluoxetine. It is formed from fluoxetine by the cytochrome P450 (CYP) isoforms CYP2C9, CYP2C19, and CYP3A. Norfluoxetine inhibits serotonin (5-HT) uptake in rat brain synaptosomal membrane preparations (Ki = 44.7 nM) and isolated human platelets (IC50 = ~15 nM). It has been found in the tissues of fish exposed to wastewa...
T40654	Avatrombopag hydrochloride AKR-501 hydrochloride,YM477hydrochloride,E5501hydrochloride
	Avatrombopag hydrochloride (AKR-501) is an orally active, nonpeptide agonist of the thrombopoietin (TPO) receptor with an EC 50 of 3.3 nM. It effectively mimics the biological activities of TPO, stimulating platelet production by activating the intracellular signaling system and facilitating the generation of platelets and megakaryocytes from hemopoietic precursor cells. Additionally, Avatrombopag hydrochloride serves as a substrate for cytochrome P450 (CYP) 2C9 and CYP3A.
T37064	6β-hydroxy Eplerenone
	6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. \|1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).
T13460	(+)-Cevimeline hydrochloride hemihydrate (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011	Others	Others
	(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。
T13421	(-)-Cevimeline hydrochloride hemihydrate (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate	ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。
T15048	Dagrocorat PF-00251802	Others	Others
	Dagrocorat is a novel and dissociated agonist of glucocorticoid receptor.

化合物

Cat.No: T22437

Synonym: LY-213829

Target: Others

2-Phenyl-2-(1-piperidinyl)propane

Cat.No: T7788

Target: Others

Cat.No: T6246

Synonym: Tybost,GS-9350,考西司他

Target: P450, HIV Protease

hCYP3A4 Fluorogenic substrate 1

Cat.No: T77698

Target: Others

Cat.No: T79343

Cat.No: T63954

Cat.No: T64032

Cat.No: T64037

Cat.No: T13600

Synonym: 4-nitro-1-trityl-1H-imidazole

Target: P450

Cat.No: T13601

Synonym: 1-TRITYL-1H-IMIDAZOL-4-AMINE

Target: P450

Pregnenolone Carbonitrile

Cat.No: T21818

Synonym: Pregnenolone 16α-carbonitrile ,5-Pregnen-3β-ol-20-one-16α-carbonitrile

Target: P450

Cat.No: T22025

Target: P450, GNRH Receptor

Cat.No: T0120

Synonym: UK-109496,伏立康唑

Target: Antifection, Antifungal

16α-Hydroxyprednisolone

Cat.No: T8339

Synonym: 16alpha-羟基泼尼松龙,16alpha-Hydroxyprednisolone

Target: Others, Drug Metabolite

Cat.No: T21548

Synonym: CYP3cide

Target: P450

Phenoprolamine Hydrochloride

Cat.No: T28400

Synonym: phenoprolamine,DDPH

Dihydrodiol-Ibrutinib

Cat.No: T36429

Desmethyl Ranolazine

Cat.No: T36723

Desethylamiodarone hydrochloride

Cat.No: T11002

Synonym: N-desethylamiodarone hydrochloride,LB 33020 hydrochloride

Target: Others

Norfluoxetine-d5 HCl

Cat.No: T71302

Avatrombopag hydrochloride

Cat.No: T40654

Synonym: AKR-501 hydrochloride,YM477hydrochloride,E5501hydrochloride

6β-hydroxy Eplerenone

Cat.No: T37064

(+)-Cevimeline hydrochloride hemihydrate

Cat.No: T13460

Synonym: (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011

Target: Others

(-)-Cevimeline hydrochloride hemihydrate

Cat.No: T13421

Synonym: (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate

Target: ALK

Cat.No: T15048

Synonym: PF-00251802

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T19792	1,3,7-Trimethyluric acid	Others	Others
	1,3,7-Trimethyluric acid 是咖啡因的代谢产物。其与咖啡因的代谢比可以反映 CYP3A 活性的变化情况。
T2926	Schizandrin A	P450; Virus Protease; Autophagy	Autophagy; Metabolism; Microbiology/Virology
	Schisandrin A 是一种从东方药物五味子中提取的主要有效成分，抑制 CYP3A 活性，IC50 分别为 6.60 μM 和 Ki 为 5.83 μM。
T6S0119	Dauricine 蝙蝠葛碱	Apoptosis; Others; NF-κB	Apoptosis; NF-κB; Others
	Dauricine 是存在于北豆根粉末中的一种双苯异喹啉生物碱，具有抗炎活性。它通过抑制NF-κB 激活，剂量依赖性地抑制结肠癌细胞的增值和侵袭，并诱导凋亡。
T6S1917	Schisandrol B Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B	P450; Reactive Oxygen Species; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Schisandrol B (Besigomsin) 是华中五味子的主要活性成分，具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生，也抑制 P-糖蛋白和CYP3A 的活性。
TN3146	6',7'-Dihydroxybergamottin acetonide	Others	Others
	6',7'-Dihydroxybergamottin is a potent inhibitor of CYP3A activity, and may be primarily responsible for the effects of grapefruit juice on cytochrome P450 activity in humans.

天然产物

1,3,7-Trimethyluric acid

Cat.No: T19792

Target: Others

Cat.No: T2926

Target: P450, Virus Protease, Autophagy

Cat.No: T6S0119

Synonym: 蝙蝠葛碱

Target: Apoptosis, Others, NF-κB

Cat.No: T6S1917

Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

Target: P450, Reactive Oxygen Species, Autophagy

6',7'-Dihydroxybergamottin acetonide

Cat.No: TN3146

Target: Others

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