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Search Results for " cyp1a2 "

31

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0778	Phenacetin 非那西丁,Acetophenetidin	COX	Immunology/Inflammation; Neuroscience
	Phenacetin (Acetophenetidin) 是一种非阿片类解热化合物，可用于缓解疼痛的研究。它是一种选择性的COX-3抑制剂，能作为人肝微粒体和大鼠体内 CYP1A2 的探针。
T7699	AZD7325 AZD-7325	P450; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	AZD7325 (AZD-7325) 是具有口服活性的α2和α3受体正向别构调节剂，Ki 分别是 0.3 和 1.3 nM。它是中等 CYP1A2和强效 CYP3A4诱导剂，有用于焦虑和 dravet 综合征相关的研究潜力。
T50053	Lofemizole	P450	Metabolism
	Lofemizole 是 CYP1A2 的拮抗剂。
T7696	3-Cyano-7-ethoxycoumarin	Others	Others
	3-Cyano-7-ethoxycoumarin 是荧光色素 P-450底物，在酶切时获得蓝色荧光产物。
T35716	N-desmethyl Olanzapine 4'-Desmethylolanzapine	P450; Drug Metabolite	Metabolism
	N-desmethyl Olanzapine 是一种非典型抗精神病化合物Olanzapinec 的代谢产物，是通过细胞色素 450（CYP）同工酶 CYP1A2 对奥氮平进行氧化代谢而形成的。
T3585	TMS (E)-2,3',4,5'-tetramethoxystilbene,2,3',4,5'-Tetramethoxystilbene	P450	Metabolism
	TMS (2,3',4,5'-Tetramethoxystilbene) 是一种白藜芦醇的甲基化衍生物，也是具有选择性的CYP1B1竞争性抑制剂，其IC50=6 nM，Ki=3 nM。它对 CYP1A1 (IC50:300 nM) 及 CYP1A2 (IC50:3.1 μM) 的抑制作用较小。它具有抗癌作用。
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。
T3424	Ezutromid BMN 195,VOX-C1100,依珠曲米,SMT C1100	Others	Others
	Ezutromid (BMN 195) 是一种具有口服活性的、首创的苯并恶唑 utrophin 调节剂，EC50=0.91 μM。它抑制人肝微粒体 CYP1A2 酶活性，IC50=5.4 μM。它可用于 Duchenne 型肌营养不良症 (DMD) 的研究。
T7410	Furafylline 呋拉茶碱,呋喃茶碱	P450	Metabolism
	Furafylline 是有选择性的人细胞色素P450IA2抑制剂(IC50:0.07 μM)。
T12806	(S)-Mirtazapine D3 (S)-Org3770 D3,(S)-6-Azamianserin D3	5-HT Receptor	GPCR/G Protein; Neuroscience
	(S)-Mirtazapine D3 is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a stereoselective antagonist of 5-HT2 receptor. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.
T9704	1-Ethynylpyrene	P450	Metabolism
	1-Ethynylpyrene 是有效的细胞色素P450 1A1, 1A2和2B1抑制剂，抑制的IC50分别为 0.18，0.32 和 0.04 μM。
T35919	N-hydroxy Riluzole
	N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique, B., Stevens, J., et al.Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitroJ. Pharmacol. Exp. Ther.282(3)1465-1472(1997)
T73039	CYP1B1-IN-3
	CYP1B1-IN-3为选择性CYP1B1抑制剂，其IC50值分别针对CYP1B1、CYP1A1、CYP1A2为6.6, 347.3, >10000 nM。该化合物能够抑制细胞迁移与侵袭，并作用于P-gp、AKT/ERK、FAK/SRC及EMT信号通路。
T37430	Mirtazapine N-oxide
	Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes.
T73042	CYP1B1-IN-5	P450	Metabolism
	CYP1B1-IN-5 是一种具有选择性和高效性的细胞色素 P450 1B1 (CYP1B1) 抑制剂，IC50 为 4.7 nM。CYP1B1-IN-5 可用于研究与代谢相关的疾病。
T82194	HIV-IN-9
	HIV-IN-9 (Compound 2b)为一种HIV抑制剂，IC50值为6.65 μg/mL，对HIV-RT展现出高度结合亲和力。此外，HIV-IN-9亦能抑制CYP3A4、CYP1A2、CYP2C1和CYP2D6等多种酶。
T74519	PROTAC CYP1B1 degrader-1
	PROTACCYP1B1 degrader-1 (Compound 6C) 是一种 α-萘黄酮嵌合衍生物，能够通过靶向 CYP1B1降解消除细胞色素 P450 (CYP)1B1 介导的耐药性，对 CYP1B1 和 CYP1A2 的 IC50分别为 95.1 和 9838.6 nM。PROTACCYP1B1 Degrader-1 可用于研究 CYP1B1过表达的前列腺癌。
T24135	HEC72702 HEC-72702,HEC 72702
	HEC72702 is a novel Hepatitis B virus capsid inhibitor, based on clinical candidate GLS4. HEC72702 was found to display no induction of the CYP1A2, CYP3A4, or CYP2B6 enzyme at the high concentration of 10 μM.
T2753	Avasimibe PD-148515,阿伐麦布,CI-1011	P450; Acyltransferase	Metabolism
	Avasimibe (PD-148515) 是一种口服有效的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂，对 ACAT1和 ACAT2的 IC50分别为 24 和 9.2 µM。Avasimibe 在前列腺癌中有研究的价值。
T62825	URAT1 inhibitor 2
	URAT1 inhibitor 2 是一种口服具有活力的 URAT1 和 CYP isozyme 抑制剂，对 URAT1 介导的 14C-UA 吸收、CYP1A2、CYP2C9 的 IC50 值分别为 1.36 μM、16.97 μM、5.22 μM。URAT1 inhibitor 2 是一种有前途的、能够用于研究高尿酸血症和痛风的候选药物。
T70786	ML252
	ML252是一种钾离子通道(potassium channel)的选择性抑制剂，主要针对KCNQ2 (Kv7.2，IC50=69 nM)。同时，ML252对细胞色素Cytochrome P450也有抑制作用，其IC50值分别为CYP1A2为6.1 nM、CYP2C9为18.9 nM、CYP3A4为3.9 nM、CYP2D6为19.9 nM。
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。
T37211	5-hydroxy-6-methoxy (S)-Duloxetine
	5-hydroxy-6-methoxy (S)-Duloxetine is a metabolite of (S)-duloxetine . It is formed from (S)-duloxetine via a 5- or 6-hydroxy duloxetine intermediate, which is formed by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6, and a catechol duloxetine intermediate. 5-hydroxy-6-methoxy (S)-Duloxetine binds to the serotonin (5-HT), norepinephrine, and dopamine transporters with Ki values of 266, 920, and 2,814 nM, respectively.
T69758	Flutamide-d7
	Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 µM, respectively. Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft mo...
T38581	Antofloxacin
	Antofloxacin is a well-tolerated, orally active, and broad-spectrum 8-amino-fluoroquinolone compound that exhibits potent antibacterial properties. It demonstrates superior activity against gyrA mutation-positive Helicobacter pylori strains, particularly in strains with mutations in the Asn87 position, when compared to levofloxacin. Additionally, Antofloxacin acts as a weak but reversible inhibitor of CYP1A2 and is clinically used to treat infections caused by various bacterial species.
T35681	MeIQx
	MeIQx (MeIQx) is a food-derived carcinogen that has been found in high temperature-cooked fish and meats.1It is activated by hydroxylation and subsequent O-acetylationviathe cytochrome P450 (CYP) isoform CYP1A2 and N-acetyltransferase 2, respectively, in UV5 cells expressing the human enzymes to a metabolite that reacts with DNA to form adducts.2MeIQx (200 and 400 ppm in the diet) induces tumor formation in rats.3
T71327	Paraxanthine-d6
	Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agoni...
T83888	(S)-5-hydroxy-6-methoxy Duloxetine maleate
	(S)-5-羟基-6-甲氧基Duloxetine是(S)-duloxetine的一个活性代谢物，主要通过对血清素(5-HT)和去甲肾上腺素的再摄取进行抑制。它通过(S)-duloxetine经过一个5-或6-羟基Duloxetine中间体以及一个儿茶酚Duloxetine中间体形成，这些中间体由细胞色素P450 (CYP)同型酶CYP1A2和CYP2D6形成。(S)-5-羟基-6-甲氧基Duloxetine在脂质膜中抑制5-HT转运体(SERT)、去甲肾上腺素转运体(NET)和多巴胺转运体(DAT)，其对人类转运体的抑制常数(Kis)分别为266、920和2,814 nM。
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。
T10535L	BI 653048 phosphate	P450	Metabolism
	BI 653048 phosphate is a selective and orally active agonist of nonsteroidal glucocorticoid (GC)(IC50 : 55 nM).
T10535	BI 653048	P450	Metabolism
	BI 653048 is a selective and orally active agonist of nonsteroidal glucocorticoid (IC50: 55 nM). BI 653048 is also an HCV NS3 protease inhibitor.

化合物

Cat.No: T0778

Synonym: 非那西丁,Acetophenetidin

Target: COX

Cat.No: T7699

Synonym: AZD-7325

Target: P450, GABA Receptor

Cat.No: T50053

Target: P450

3-Cyano-7-ethoxycoumarin

Cat.No: T7696

Target: Others

N-desmethyl Olanzapine

Cat.No: T35716

Synonym: 4'-Desmethylolanzapine

Target: P450, Drug Metabolite

Cat.No: T3585

Synonym: (E)-2,3',4,5'-tetramethoxystilbene,2,3',4,5'-Tetramethoxystilbene

Target: P450

Cat.No: T4567

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

Target: P450, Antibacterial

Cat.No: T3424

Synonym: BMN 195,VOX-C1100,依珠曲米,SMT C1100

Target: Others

Cat.No: T7410

Synonym: 呋拉茶碱,呋喃茶碱

Target: P450

(S)-Mirtazapine D3

Cat.No: T12806

Synonym: (S)-Org3770 D3,(S)-6-Azamianserin D3

Target: 5-HT Receptor

1-Ethynylpyrene

Cat.No: T9704

Target: P450

N-hydroxy Riluzole

Cat.No: T35919

Cat.No: T73039

Mirtazapine N-oxide

Cat.No: T37430

Cat.No: T73042

Target: P450

Cat.No: T82194

PROTAC CYP1B1 degrader-1

Cat.No: T74519

Cat.No: T24135

Synonym: HEC-72702,HEC 72702

Cat.No: T2753

Synonym: PD-148515,阿伐麦布,CI-1011

Target: P450, Acyltransferase

URAT1 inhibitor 2

Cat.No: T62825

Cat.No: T70786

Cat.No: T79568

Target: Parasite

5-hydroxy-6-methoxy (S)-Duloxetine

Cat.No: T37211

Cat.No: T69758

Cat.No: T38581

Cat.No: T35681

Paraxanthine-d6

Cat.No: T71327

(S)-5-hydroxy-6-methoxy Duloxetine maleate

Cat.No: T83888

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

Cat.No: T7788

Target: Others

BI 653048 phosphate

Cat.No: T10535L

Target: P450

Cat.No: T10535

Target: P450

Cat. No.	Product Name	Target	Signaling Pathways
T37784	2,6-Dimethylquinoline	P450	Metabolism
	2,6-Dimethylquinoline 是一种从前胡根中提取的天然产物。2,6-Dimethylquinoline 是 CYP1A2 和 CYP2B6 的抑制剂，IC50 分别为 3.3 和 480 µM。
T2949	Alizarin Mordant Red 11,Anthraquinonic,茜素	P450	Metabolism
	Alizarin (Mordant Red 11) 是一种天然红色染料，从茜草植物根部提取得到，已广泛用作纺织品和绘画中的颜料。
TN3013	4,5-Dimethoxycanthin-6-one Methylnigakinone	P450; Antibacterial; PDE	Metabolism; Microbiology/Virology
	4,5-Dimethoxycanthin-6-one 从 Picrasma quassioides BENNET (Simaroubaceae)是一种从 Picrasma quassioides BENNET (Simaroubaceae) 中分离得到生物碱。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（IC50 ： 1.7 μM, Ki ： 2.6 μM），对环磷酸腺苷（cAMP）磷酸二酯酶有很强的抑制作用。4,5-Dimethoxycanthin-6-one 具有抗菌活性，对金黄色葡萄球菌及其耐药菌株有抑制作用。4,5-Dimethoxycanthin-6-one 对肿瘤细胞株 U937 和 HepG2 具有细胞毒性。
T11218	ε-Viniferin epsilon-Viniferin,Epsilon-白藜芦醇脱氢二聚体	P450	Metabolism
	ε-Viniferin (epsilon-Viniferin) 提取自 Vitis vinifera，是 Resveratrol 的二聚体，能够抑制 CYP 家族,其 Ki=0.5~20 μM，具有抗氧化作用。
TN1702	Glycycoumarin 甘草香豆素	P450; JNK; AMPK; Autophagy	Autophagy; Chromatin/Epigenetic; MAPK; Metabolism; PI3K/Akt/mTOR signaling
	Glycycoumarin 是甘草中的一种香豆素，能直接靶向 T-LAK 细胞源蛋白激酶发挥抗肝癌活性。它通过激活自噬，抑制内质网应激介导的 JNK 和 GSK-3 介导的线粒体途径，来抑制肝细胞脂性凋亡。它是一种雌激素激动剂，对 CYP1A2 和 CYP2B6 有中度抑制作用。
T3818	Fraxinol	Others; P450	Metabolism; Others
	Fraxinol 是一种分离自半边莲中的化合物。
T7472	7-Hydroxyflavone 7-羟基黄酮,7羟基黄酮	P450	Metabolism
	7-Hydroxyflavone 是一种黄酮类化合物，从M. indica 中分离得到，具有抗炎活性。它利用 ERK/Nrf2/HO-1 通路保护肾细胞，使其免受尼古丁诱导的细胞毒性。
T2878	Ginsenoside Rd Panaxoside Rd,Sanchinoside Rd,人参皂苷Rd,人参皂苷 Rd,Gypenoside VIII	P450; Calcium Channel; NF-κB; COX; Endogenous Metabolite	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; NF-κB
	Ginsenoside Rd (Gypenoside VIII) 抑制 TNFα 诱导的NF-κB 转录活性，还抑制COX-2和iNOSmRNA 的表达。它抑制CYP2D6、CYP1A2、CYP3A4和CYP2C9，也抑制Ca2+内流，有可能抑制或阻止肿瘤生长。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。
T5582	β-Apo-8'-carotenal ψ-胡萝卜醛,trans-β-apo-8'-carotenal,BETA-阿朴-8'-胡萝卜醛,Apocarotenal	Others; P450	Metabolism; Others
	β-Apo-8'-carotenal (Apocarotenal) 是一种存在于许多蔬菜、水果中的维生素原 A 类胡萝卜素，是大鼠CYP1A1和CYP1A2的诱导剂。
TN5901	Cudratricusxanthone A
	Cudratricusxanthone A has potent anti-proliferative, antioxidative, and monoamine oxidase inhibitory effects, it also possesses anti-cancer activities and provide a basis for developing effective therapeutic agents to inhibit growth and metastasis of brea

天然产物

2,6-Dimethylquinoline

Cat.No: T37784

Target: P450

Cat.No: T2949

Synonym: Mordant Red 11,Anthraquinonic,茜素

Target: P450

4,5-Dimethoxycanthin-6-one

Cat.No: TN3013

Synonym: Methylnigakinone

Target: P450, Antibacterial, PDE

Cat.No: T11218

Synonym: epsilon-Viniferin,Epsilon-白藜芦醇脱氢二聚体

Target: P450

Cat.No: TN1702

Synonym: 甘草香豆素

Target: P450, JNK, AMPK, Autophagy

Cat.No: T3818

Target: Others, P450

7-Hydroxyflavone

Cat.No: T7472

Synonym: 7-羟基黄酮,7羟基黄酮

Target: P450

Cat.No: T2878

Synonym: Panaxoside Rd,Sanchinoside Rd,人参皂苷Rd,人参皂苷 Rd,Gypenoside VIII

Target: P450, Calcium Channel, NF-κB, COX, Endogenous Metabolite

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

β-Apo-8'-carotenal

Cat.No: T5582

Synonym: ψ-胡萝卜醛,trans-β-apo-8'-carotenal,BETA-阿朴-8'-胡萝卜醛,Apocarotenal

Target: Others, P450

Cudratricusxanthone A

Cat.No: TN5901

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