首页工具

登录

搜索结果

Search Results for " cyp2d6 "

33

抑制剂 & 化合物

12

天然产物

如果没找到您满意的产品或者您对产品有其他要求，可以联系我们专业顾问为您提供针对性的合理建议。 QQ咨询网站留言咨询

Cat. No.	Product Name	Target	Signaling Pathways
T16369	O-Desmethyl gefitinib	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	O-Desmethyl gefitinib 是依赖于 CYP2D6 活性形成的，是 Gefitinib 在人血浆中的活性代谢产物。在亚细胞试验中，它抑制 EGFR，IC50为 36 nM。
T28827	Sofpironium bromide BBI4000,BBI 4000,BBI-4000	Others; AChR	Neuroscience; Others
	Sofpironium bromide (BBI4000) 是一种抗胆碱能剂，用于研究原发性腋窝多汗症。它对 M1、M2、M4 和 M5 亚型也有很高的亲和力。它通过抑制应用部位外分泌腺中的M3毒蕈碱受体来减少出汗。
T10989	Dehydroaripiprazole OPC-14857,DM-14857	5-HT Receptor	GPCR/G Protein; Neuroscience
	Dehydroaripiprazole (DM-14857) 是 Aripiprazole 的活性代谢产物，具有抗精神病活性。Aripiprazole 是也一种抗精神病药。
T10335	Antihistamine-1	P450	Metabolism
	Antihistamine-1 是能够渗透血脑屏障的 H1-抗组胺药 (Ki=6.9 nM), 它也是 CYP2D6 和 hERG 通道的抑制剂，其 IC50 值分别为 5.4 和 0.8 μM。
T4281	Endoxifen (E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen	Estrogen Receptor/ERR; Aromatase; Estrogen/progestogen Receptor; Parasite; Drug Metabolite	Endocrinology/Hormones; Metabolism; Microbiology/Virology
	Endoxifen ((E/Z)-Endoxifen) 是 Tamoxifen 的关键活性代谢物，能抑制芳香酶的活性，与雌激素受体有较高的亲和力和特异性。它有潜力研究乳腺癌。
T34795	Tedatioxetine Lu AA 24530,Lu AA-24530,Lu AA24530	Dopamine Receptor; Serotonin Transporter	GPCR/G Protein; Neuroscience
	Tedatioxetine (Lu AA24530) 是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂（SNDRI），具有抗抑郁作用。Tedatioxetine 可作为 CYP2D6 底物。
T8182L	Guan-fu base A hydrochloride(1394-48-5 free base)	P450	Metabolism
	Guan-fu base A hydrochloride(1394-48-5 free base) 是一种从乌头中分离得到的抗心律失常生物碱。它是一种 CYP2D6 人类、猴子和狗同工型的抑制剂。
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。
T1443	Memantine hydrochloride 3,5-二甲基金刚胺盐酸盐,盐酸美金刚,Namenda,Memantine HCl,D-145 (hydrochloride)	P450; GluR; NMDAR; Autophagy; iGluR	Autophagy; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Memantine hydrochloride (Memantine HCl) 是一种具有一些多巴胺能作用的金刚烷胺衍生物，是一种温和的 NMDA 受体非竞争性拮抗剂，能够抑制 CYP2B6 和 CYP2D6。它可作为抗帕金森剂。
T4488	GSK-25 GSK25	ROCK; S6 Kinase; mTOR	Cell Cycle/Checkpoint; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	GSK-25 是一种选择性的，具有口服活性的 ROCK1抑制剂。它对 31 种激酶以及 RSK1 和 p70S6K 保持良好的选择性，RSK1的 IC50 为 398 nM，p70S6K 的 IC50 为 1000nM。它可抑制 P450，对 CYP2C9、CYP2D6和 CYP3A4的 IC50分别为2.5、5.2和2.5 μM。
T50001	Tinoridine ethyl 2-amino-6-benzyl-4H,5H,6H,7H-thieno[2,3-c]pyridine-3-carboxylate,替诺立定	P450	Metabolism
	Tinoridine 通过抑制环氧合酶-2（COX-2）的产生来发挥作用，具有抗炎、抗过敏和抗凝血等活性。
T68531	MCV-4527 hydrochloride
	MCV-4527 hydrochloride is a new designer drug used as a potent inhibitor of CYP2D6.
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.
T71926	Melperone hydrochloride
	Melperone hydrochloride is a butyrophenone neuroleptic and an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine.
T10145	4-Hydroxyatomoxetine	Others	Others
	4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.
T83896	Promethazine Sulfoxide
	普罗米赛因硫醚是组胺H1受体拮抗剂普罗米赛因的代谢产物，通过细胞色素P450（CYP）亚型CYP2D6作用从普罗米赛因形成。
T21684	Bufuralol (hydrochloride)
	Bufuralol hydrochloride (Ro 3-4787 hydrochloride) 是一种有效的非选择性，口服活性的 β-肾上腺素受体 (β-adrenoreceptor) 拮抗剂，具有部分激动剂活性。Bufuralol hydrochloride 是CYP2D6 探针的底物。
T69094	α-hydroxy Metoprolol
	α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol. It is formed via metabolism of metoprolol by the cytochrome P450 (CYP) isoform CYP2D6.
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。
T36664	Dehydro Aripiprazole (hydrochloride)
	Dehydro aripiprazole is the primary, active metabolite of aripiprazole, an atypical antipsychotic. The metabolite is produced from the parent compound by the actions of cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6. Dehydro aripiprazole has similar pharmacological properties to aripiprazole.
T10144	4-Hydroxyatomoxetine D3	Others	Others
	4-Hydroxyatomoxetine D3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.
T37360	6-O-desmethyl Donepezil
	6-O-desmethyl Donepezil is an active metabolite of the acetylcholinesterase inhibitor donepezil . It is formed through dealkylation by the cytochrome P450 (CYP) isoform CYP2D6. It inhibits human ether a go-go (hERG) channels (IC50 = 1.5 μM in HEK293 cells expressing hERG).
T61515	5-HT7 receptor ligand 1
	5-HT7 receptor ligand 1 (Compound 5c) is a potent ligand for the 5-HT7 receptor, with a K i value of 8 nM. The compound demonstrates non-hepatotoxic properties and displays moderate potential for drug-drug interactions with substrates of CYP3A4 or CYP2D6 enzymes [1].
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.
T71578	Endoxifen mesylate
	Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromat...
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。
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 ...
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。
T15048	Dagrocorat PF-00251802	Others	Others
	Dagrocorat is a novel and dissociated agonist of glucocorticoid receptor.
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.
T79754	JNK-IN-14	JNK	MAPK
	JNK-IN-14是一种激酶（JNK1/2/3）抑制剂，IC50值为1.81、12.7和10.5 nM。它能诱导早期apoptosis，并在G2/M阶段引起细胞周期阻滞。与SP600125相比，在K562白血病细胞中，JNK-IN-14更强有效地抑制了Beclin-1的表达。
T16097	MK-8318	Others	Others
	MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

化合物

O-Desmethyl gefitinib

Cat.No: T16369

Target: EGFR

Sofpironium bromide

Cat.No: T28827

Synonym: BBI4000,BBI 4000,BBI-4000

Target: Others, AChR

Dehydroaripiprazole

Cat.No: T10989

Synonym: OPC-14857,DM-14857

Target: 5-HT Receptor

Antihistamine-1

Cat.No: T10335

Target: P450

Cat.No: T4281

Synonym: (E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen

Target: Estrogen Receptor/ERR, Aromatase, Estrogen/progestogen Receptor, Parasite, Drug Metabolite

Cat.No: T34795

Synonym: Lu AA 24530,Lu AA-24530,Lu AA24530

Target: Dopamine Receptor, Serotonin Transporter

Guan-fu base A hydrochloride(1394-48-5 free base)

Cat.No: T8182L

Target: P450

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

Cat.No: T7788

Target: Others

Memantine hydrochloride

Cat.No: T1443

Synonym: 3,5-二甲基金刚胺盐酸盐,盐酸美金刚,Namenda,Memantine HCl,D-145 (hydrochloride)

Target: P450, GluR, NMDAR, Autophagy, iGluR

Cat.No: T4488

Synonym: GSK25

Target: ROCK, S6 Kinase, mTOR

Cat.No: T50001

Synonym: ethyl 2-amino-6-benzyl-4H,5H,6H,7H-thieno[2,3-c]pyridine-3-carboxylate,替诺立定

Target: P450

MCV-4527 hydrochloride

Cat.No: T68531

(S)-Mirtazapine D3

Cat.No: T12806

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

Target: 5-HT Receptor

Melperone hydrochloride

Cat.No: T71926

4-Hydroxyatomoxetine

Cat.No: T10145

Target: Others

Promethazine Sulfoxide

Cat.No: T83896

Bufuralol (hydrochloride)

Cat.No: T21684

α-hydroxy Metoprolol

Cat.No: T69094

Cat.No: T82194

Dehydro Aripiprazole (hydrochloride)

Cat.No: T36664

4-Hydroxyatomoxetine D3

Cat.No: T10144

Target: Others

6-O-desmethyl Donepezil

Cat.No: T37360

5-HT7 receptor ligand 1

Cat.No: T61515

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

Cat.No: T37211

Endoxifen mesylate

Cat.No: T71578

Cat.No: T70786

(E)-10-Hydroxynortriptyline

Cat.No: T38131

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

Cat.No: T83888

Cat.No: T15048

Synonym: PF-00251802

Target: Others

BI 653048 phosphate

Cat.No: T10535L

Target: P450

Cat.No: T10535

Target: P450

Cat.No: T79754

Target: JNK

Cat.No: T16097

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T10835	Cletoquine Desethylhydroxychloroquine	Parasite; Antifection	Microbiology/Virology
	Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用，并具有治疗自身免疫性疾病的潜力。
T8182	Guanfu base A Guan-fu base A,关附甲素	P450; Potassium Channel; HER	Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Metabolism; Tyrosine Kinase/Adaptors
	Guanfu base A 是一种生物碱，分离自 Aconitum coreanum，是非竞争性 CYP2D6抑制剂，对人肝微粒体 (HLM) 的 Ki 为 1.20 μM，对人重组体 (rCYP2D6) 的 Ki 为 0.37 μM。它也是 CYP2D 的有效竞争抑制剂。它还能抑制 HERG 通道电流。Guan-fu base A 具有抗心律失常的作用。
T3401	Ginsenoside F1 人参皂苷 F1,20(S)-Ginsenoside F1	P450; Endogenous Metabolite	Metabolism
	Ginsenoside F1 (20(S)-Ginsenoside F1) 是一种 Ginsenoside Rg1 的酶促修饰衍生物，它竞争性抑制CYP3A4，对 CYP2D6 具有较弱的抑制作用。
TQ0296L	N-Nornuciferine hydrochloride(4846-19-9 free base) N-Nornuciferine hydrochloride	P450	Metabolism
	N-Nornuciferine hydrochloride(4846-19-9 free base) (N-Nornuciferine hydrochloride) 是荷叶中的一种 aporphine 生物碱，显着抑制 CYP2D6（IC50：3.76 μM，Ki：2.34 μM）。
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。
T5S2361	Epiberberine	ERK; Beta-Secretase; MEK; BACE; AMPK; AChR; AChE	Chromatin/Epigenetic; MAPK; Neuroscience; PI3K/Akt/mTOR signaling
	Epiberberine 是一种从黄连中得到的生物碱，是AChE 和BChE 抑制剂，和非竞争性BACE1抑制剂。在 3T3-L1 细胞分化早期，它能够下调 Raf/MEK1/2/ERK1/2 和 AMPKα/Akt 信号通路。它具有抗氧化作用，能够清除 ONOO-，可用于阿尔滋海默症和糖尿病的研究。
T3736	Olivetol 橄榄醇,5-Pentylresorcinol,5-n-Amylresorcinol,3,5-二羟基戊苯	Cannabinoid Receptor; P450; IκB/IKK	GPCR/G Protein; Metabolism; NF-κB
	Olivetol (5-n-Amylresorcinol) 是天然多酚类化合物，存在于地衣中，或由一些昆虫产生。它竞争性地抑制大麻素受体CB1和CB2，抑制 CYP2C19 (IC50=15.3 μM;Ki=7.21 μM) 和 CYP2D6 (IC50=2.71 μM;Ki=2.87 μM) 的活性。
TQ0296	N-Nornuciferine	P450	Metabolism
	N-Nornuciferine, an aporphine alkaloid in lotus leaf, significantly inhibits CYP2D6 (IC50: 3.76 μM, Ki: 2.34 μM).
TQ0109	Cephaeline dihydrochloride (-)-Cephaeline dihydrochloride,盐酸吐根酚碱,NSC 32944	P450	Metabolism
	(-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM).
TN1210	2-Hydroxy-1-Methoxyaporphine	P450	Metabolism
	2-Hydroxy-1-Methoxyaporphine can inhibit CYP2D6 activity, it also increase the glucose consumption significantly as rosiglitazone.
T3852	Rhodiosin	Antioxidant; AChE	Neuroscience; oxidation-reduction
	Rhodiosin 是从红景天的根中分离的特异性非竞争性细胞色素 P450 2D6 抑制剂，IC50=0.761 μM，Ki=0.769 μM。它有 DPPH 自由基清除活性，IC50=27.7 μM。它抑制乙酰胆碱酯酶，IC50范围为 57.50 至 2.43 μg/mL。
TN1011	Rhodionin	P450; AChE	Metabolism; Neuroscience
	Rhodionin 是从红景天的根中分离的特异性非竞争性细胞色素 P450 2D6 抑制剂，IC50=0.761 μM，Ki=0.769 μM。它有 DPPH 自由基清除活性，IC50为 19.49 μM。它抑制乙酰胆碱酯酶，IC50范围为 57.50 至 2.43 μg/mL。

天然产物

Cat.No: T10835

Synonym: Desethylhydroxychloroquine

Target: Parasite, Antifection

Cat.No: T8182

Synonym: Guan-fu base A,关附甲素

Target: P450, Potassium Channel, HER

Cat.No: T3401

Synonym: 人参皂苷 F1,20(S)-Ginsenoside F1

Target: P450, Endogenous Metabolite

N-Nornuciferine hydrochloride(4846-19-9 free base)

Cat.No: TQ0296L

Synonym: N-Nornuciferine hydrochloride

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: T5S2361

Target: ERK, Beta-Secretase, MEK, BACE, AMPK, AChR, AChE

Cat.No: T3736

Synonym: 橄榄醇,5-Pentylresorcinol,5-n-Amylresorcinol,3,5-二羟基戊苯

Target: Cannabinoid Receptor, P450, IκB/IKK

N-Nornuciferine

Cat.No: TQ0296

Target: P450

Cephaeline dihydrochloride

Cat.No: TQ0109

Synonym: (-)-Cephaeline dihydrochloride,盐酸吐根酚碱,NSC 32944

Target: P450

2-Hydroxy-1-Methoxyaporphine

Cat.No: TN1210

Target: P450

Cat.No: T3852

Target: Antioxidant, AChE

Cat.No: TN1011

Target: P450, AChE

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Copyright © 2015-2024 TargetMol Chemicals Inc. All rights reserved. 沪ICP备20019793号-4

沪公网安备 31010602006700号

沪公网安备 31010602006700号

TargetMol Loading

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼