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Search Results for " cyp1a1 "

28

抑制剂 & 化合物

15

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T27109	CYP1A1 inhibitor 8a
	CYP1A1 inhibitor 8a is a potent and selective CYP1A1 inhibitor. It antagonizes B[a]P mediated activation of aromatic hydrocarbon receptor (AhR) in yeast cells, thereby protects human cells from CYP1A1-mediated B[a]P toxicity.
T5116	Iprodione	Others; Reactive Oxygen Species; Antifungal	Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB; Others
	Iprodione 是一种二甲酰亚胺类的高度特异性杀菌剂，能通过产生自由氧自由基引起氧化损伤。
T10270	BAY 2416964	Aryl Hydrocarbon Receptor	Immunology/Inflammation
	BAY 2416964 是一种可口服的芳基烃受体拮抗剂，IC50为 341 nM，可用于研究实体瘤。
T8729	3-(2-Naphthalenyl)-1-(3-pyridinyl)-2-propen-1-one	P450	Metabolism
	DMU2105 是一种特异性 CYP1B1 抑制剂（CYP1B1 和 CYP1A1，IC50 分别为 10 nM 和 742 nM）。
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。
T8728	DMU-2139	P450	Metabolism
	DMU2139 是一种特异性 CYP1B1 抑制剂（CYP1B1 和 CYP1A1，IC50 分别为 9 nM 和 795 nM）。
T21507	7-Ethoxyresorufin Resorufin ethyl ether,乙氧基试卤灵	P450; NO Synthase	Immunology/Inflammation; Metabolism
	7-Ethoxyresorufin (Resorufin ethyl ether) 是细胞色素 P450 (尤其是CYP1A1) 的荧光底物和竞争性抑制剂，同时对 NO 合酶具有抑制作用。
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。
T3158L	Harman hydrochloride 哈尔满盐酸盐,Harmane hydrochloride(486-84-0 Free base)	P450	Metabolism
	Harman hydrochloride 可以以 AhR 依赖性方式直接诱导 CYP1A1 基因表达，可能代表了harman 促进致突变性、共致突变性和致癌性的新机制。
T23151	Phortress NSC 710305	AhR	Immunology/Inflammation; Metabolism
	Phortress（NSC-710305）是一种强效的AhR配体，具有强大的结合亲和力，进而触发CYP1A1的转录并诱导抗肿瘤活性。
T21704	5-fluoro 203 5F-203,NSC-703786	Others	Others
	5-fluoro 203 (NSC-703786) 是一种细胞毒性分子。它可激活芳香烃受体(AhR) 信号传导，诱导 CYP1A1 的转录，从而形成 DNA 加合物以及细胞周期阻滞。它可以提高活性氧水平，并激活 ERK、p38以及JNK。
T7088	Diflubenzuron Dimilin,氟脲杀,Difubenzuron,Larvakil,Difluron	P450	Metabolism
	Diflubenzuron (Larvakil) 是杀虫剂 Dimilin 的有效成分，具有杀幼虫和杀卵作用。
T3637	Pifithrin-β hydrobromide Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)	Ferroptosis; p53	Apoptosis
	Pifithrin-β hydrobromide (Cyclic PFT-α) 是一种 p53 的抑制剂，可逆地阻断 p53 依赖性转录激活和细胞凋亡。IC50值为23 μM。
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。
T2196	Fipronil 氟虫腈,Fluocyanobenpyrazole,Termidor	P450; GluCls; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience
	Fipronil (Fluocyanobenpyrazole) 是昆虫GABA 受体的选择性拮抗剂，可抑制蟑螂神经元中谷氨酸盐引起的脱敏和非脱敏。在分离的大鼠肝微粒体中，它诱导细胞色素 P450 (CYP) 亚型CYP1A1/2、CYP2B1/2和CYP3A1/2的活性。
T73040	CYP1B1-IN-4	P450	Metabolism
	CYP1B1-IN-4为选择性CYP1B1抑制剂（IC50=0.2 nM），属2,4-二芳基噻唑类化合物。其对细胞的毒性低，且在人类及大鼠肝微粒体中表现出稳定性。
T32136	ICT2700 de OH CPI MI,deOHCPIMI,de-OH-CPI-MI,ICT 2700,ICT-2700
	ICT2700 is a potent cytotoxin selectively by CYP1A1 as a tumor-selective treatment for human bladder cancers.
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。
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。
T12449	Phortress free base	Others	Others
	Phortress free base is a P450 CYP1A1-activated antitumor prodrug with antitumor activity.
T36793	Dolutegravir M1
	Dolutegravir M1 is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed primarily by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1. 1.Zhu, J., Wang, P., Li, F., et al.CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitorBiochem. Pharmacol.158174-184(2018)
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。
T72552	Antitumor agent-88
	Antitumor agent-88 表现出有效的抗有丝分裂活性并使细胞停滞在 G2/M 期。Antitumor agent-88 扰乱表达 CYP1A1 的乳腺癌细胞中的微管和细胞骨架。Antitumor agent-88 也是 CYP1A1的竞争性抑制剂 (Ki: 1.4 μM)。
T72551	Antitumor agent-87
	Antitumor agent-87为一种有效抗肿瘤化合物，对CYP1A1具有高亲和性（Ki值0.23 µM），表现出抗增殖活性并能诱导细胞周期在G2/M期停滞，进而展现抗肿瘤活性。
T70257	Avitriptan HCl
	Avitriptan, also known as BMS-180048, is a selective 5-HT1-like receptor agonist. Avitriptan is an effective compound for the treatment of migraine headaches with a prolonged duration of response. Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.
T36039	16α-Hydroxyestrone
	The naturally-occurring estrogens are estrone , estradiol , and estriol . 16α-hydroxy Estrone (16α-OHE1) is a hydroxylated metabolite of E1 as well as an interconversion product with E2. E1 is 16α-hydroxylated by cytochrome P450 (CYP) isoforms, including CYP1A1, CYP3A5, CYP3A4, and CYP3A7, with CYP3A5 being breast-specific. 16α-OHE1 is sulphatized or glucuronidated before excretion. It is increased in rheumatoid arthritis and decreased by physical activity. Unlike the parent estrogens and other ...
T35855	AAA
	AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension...
T36215	17R(18S)-EpETE
	17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ...

化合物

CYP1A1 inhibitor 8a

Cat.No: T27109

Cat.No: T5116

Target: Others, Reactive Oxygen Species, Antifungal

Cat.No: T10270

Target: Aryl Hydrocarbon Receptor

3-(2-Naphthalenyl)-1-(3-pyridinyl)-2-propen-1-one

Cat.No: T8729

Target: P450

Cat.No: T3585

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

Target: P450

Cat.No: T8728

Target: P450

7-Ethoxyresorufin

Cat.No: T21507

Synonym: Resorufin ethyl ether,乙氧基试卤灵

Target: P450, NO Synthase

3-Cyano-7-ethoxycoumarin

Cat.No: T7696

Target: Others

Harman hydrochloride

Cat.No: T3158L

Synonym: 哈尔满盐酸盐,Harmane hydrochloride(486-84-0 Free base)

Target: P450

Cat.No: T23151

Synonym: NSC 710305

Target: AhR

Cat.No: T21704

Synonym: 5F-203,NSC-703786

Target: Others

Cat.No: T7088

Synonym: Dimilin,氟脲杀,Difubenzuron,Larvakil,Difluron

Target: P450

Pifithrin-β hydrobromide

Cat.No: T3637

Synonym: Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)

Target: Ferroptosis, p53

Cat.No: T4567

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

Target: P450, Antibacterial

Cat.No: T2196

Synonym: 氟虫腈,Fluocyanobenpyrazole,Termidor

Target: P450, GluCls, GABA Receptor

Cat.No: T73040

Target: P450

Cat.No: T32136

Synonym: de OH CPI MI,deOHCPIMI,de-OH-CPI-MI,ICT 2700,ICT-2700

1-Ethynylpyrene

Cat.No: T9704

Target: P450

Cat.No: T73039

Phortress free base

Cat.No: T12449

Target: Others

Dolutegravir M1

Cat.No: T36793

Cat.No: T73042

Target: P450

Antitumor agent-88

Cat.No: T72552

Antitumor agent-87

Cat.No: T72551

Cat.No: T70257

16α-Hydroxyestrone

Cat.No: T36039

Cat.No: T35855

Cat.No: T36215

Cat. No.	Product Name	Target	Signaling Pathways
T8198	Visnagin	Others	Others
	Visnagin 是一种抗氧化剂呋喃香豆素衍生物。它具有预防Cerulein 诱导的急性胰腺炎的潜力。它在血管平滑肌中具有良好的血管扩张作用。它具有抗炎作用，可用于缓解疼痛的研究。
T5786	TETRAHYDROPIPERINE 四氢胡椒碱,Cosmoperine	P450; TRP/TRPV Channel	Membrane transporter/Ion channel; Metabolism
	Tetrahydropiperine (Cosmoperine) 是胡椒碱的环己基类似物，也是一种天然芳基戊酰胺，从Piper longum 分离得到。它对细胞色素 P450 (CYP) 同工型 CYP1A1/芳基烃羟化酶 (AHH；IC50=23 µM)具有抑制作用。
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。
T3668	Galangin Norizalpinin,高良姜素,3,5,7-Trihydroxyflavone	ERK; P450; NF-κB; Autophagy	Autophagy; MAPK; Metabolism; NF-κB
	Galangin (Norizalpinin) 是芳烃受体的激动剂/拮抗剂，并且还显示对 CYP1A1 活性的抑制作用。
T9328	Ellagic Acid Dihydrate	P450	Metabolism
	Ellagic Acid Dihydrate 抑制 CYP1A1 依赖的benzo[a]pyrene 活化。
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。
T5S0669	Bergamottin 5-Geranoxypsoralen,Bergamotine,Bergaptin,佛手柑素	P450	Metabolism
	Bergamottin (5-Geranoxypsoralen) 是竞争性CYP1A1抑制剂(Ki:10.703 nM)。
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。
TN1724	Harmalol hydrochloride Harmidol hydrochloride	P450; Antioxidant	Metabolism; oxidation-reduction
	Harmalol hydrochloride (Harmidol hydrochloride) 是一种可从Peganum harmala L.的种子中提取出来的β-咔啉生物碱。Harmalol hydrochloride 是Harmaline 的主要代谢产物，在转录和翻译后水平上显著抑制二恶英介导的 CYP1A1 诱导。Harmalol hydrochloride 在去氧肾上腺素或KCl 预先收缩的分离大鼠胸主动脉制剂中显示出血管松弛活性。 Harmalol hydrochloride 具有抗氧化活性.
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。
TN1222	26-Deoxyactein 27-Deoxyactein,脱氧升麻烃,23-epi-26-Deoxyactein,27-脱氧升麻亭	NOS; CDK; NO Synthase	Cell Cycle/Checkpoint; Immunology/Inflammation
	23-epi-26-Deoxyactein (27-Deoxyactein) 是一种黑升麻中的主要成分，能够阻止 TCDD 诱导的成骨细胞的损伤。它对 AhR，CYP1A1 和 ERK 的水平升高具有抑制作用。
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。
TQ0276	Methysticin DL-Methysticin,麻醉椒苦素,(±)-Methystici	P450	Metabolism
	Methysticin, a major kavalactone extracted from kava, can induce CYP1A1.
T3776	Rhapontigenin 丹叶大黄素,Protigenin	P450; Antibacterial; Antifungal	Metabolism; Microbiology/Virology
	Rhapontigenin (Protigenin) 是一种基于机制的选择性细胞色素 P450 1A1 (IC50: 400 nM) 灭活剂。它是一种芳烃羟化酶，可激活作为致癌物质的多环芳烃。它是白藜芦醇的天然类似物，具有抗癌，抗氧化剂，抗真菌和抗菌活性。
T13670L	(Z)-Ligustilide 藁本内酯,cis-Ligustilide,Ligustilide A,蒿本内酯 A	Antibacterial	Microbiology/Virology
	(Z)-Ligustilide (Ligustilide A) 是从川芎中提取的天然产物，具有抗菌和抗真菌活性。它抑制 FATP5 和 DGAT 的表达，抑制小鼠脂肪酸的摄取和酯化，有潜力研究非酒精性脂肪性肝病。

天然产物

Cat.No: T8198

Target: Others

TETRAHYDROPIPERINE

Cat.No: T5786

Synonym: 四氢胡椒碱,Cosmoperine

Target: P450, TRP/TRPV Channel

Cat.No: T2949

Synonym: Mordant Red 11,Anthraquinonic,茜素

Target: P450

Cat.No: T3668

Synonym: Norizalpinin,高良姜素,3,5,7-Trihydroxyflavone

Target: ERK, P450, NF-κB, Autophagy

Ellagic Acid Dihydrate

Cat.No: T9328

Target: P450

7-Hydroxyflavone

Cat.No: T7472

Synonym: 7-羟基黄酮,7羟基黄酮

Target: P450

Cat.No: T5S0669

Synonym: 5-Geranoxypsoralen,Bergamotine,Bergaptin,佛手柑素

Target: P450

Cat.No: T11218

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

Target: P450

Harmalol hydrochloride

Cat.No: TN1724

Synonym: Harmidol hydrochloride

Target: P450, Antioxidant

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

Cat.No: TN1222

Synonym: 27-Deoxyactein,脱氧升麻烃,23-epi-26-Deoxyactein,27-脱氧升麻亭

Target: NOS, CDK, NO Synthase

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

Cat.No: TQ0276

Synonym: DL-Methysticin,麻醉椒苦素,(±)-Methystici

Target: P450

Cat.No: T3776

Synonym: 丹叶大黄素,Protigenin

Target: P450, Antibacterial, Antifungal

(Z)-Ligustilide

Cat.No: T13670L

Synonym: 藁本内酯,cis-Ligustilide,Ligustilide A,蒿本内酯 A

Target: Antibacterial

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