首页工具

登录

搜索结果

Search Results for " cyp450 "

42

抑制剂 & 化合物

3

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
T1787	Levobupivacaine	Sodium Channel	Membrane transporter/Ion channel
	Levobupivacaine 是一种氨基酰胺类局麻药，属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。
T22394	Paritaprevir ABT450,ABT-450,帕利普韦,Veruprevir	HCV Protease	Microbiology/Virology; Proteases/Proteasome
	Paritaprevir (ABT450) 是一种非结构蛋白 3/4A 蛋白酶抑制剂，对 HCV 1a 和 HCV 1b 的 EC50 值分别为 1 和 0.21 nM。它也是SARS-CoV 3CLpro 的抑制剂，IC50为 1.31 μM。
T6566	Levobupivacaine hydrochloride Levobupivacaine HCl,(S)-(-)-Bupivacaine HCl,盐酸左布比卡因,(S)-(-)-Bupivacaine monohydrochloride	Sodium Channel	Membrane transporter/Ion channel
	Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) 是有效的钠通道阻滞剂。
T22003	2,3-dihydrothieno-Thiadiazole Carboxylate	P450	Metabolism
	2,3-dihydrothieno-Thiadiazole Carboxylate 是一种 CYP450（CYP2E1 和 CYP2B4）抑制剂。
T20373	1-Phenylpyrrole NSC16581,NSC-16581,1-苯基吡咯,NSC 16581	Others	Others
	1-Phenylpyrrole (NSC-16581) 可抑制大鼠肝脏微粒体中 CYP450 依赖性单加氧酶活性。
T4983	Isoetharine mesylate salt Isoetarine mesilate,异丙肾上腺素甲磺酸盐	Others; Adrenergic Receptor	GPCR/G Protein; Neuroscience; Others
	Isoetharine mesylate salt (Isoetarine mesilate) 是一种 β-肾上腺素能受体激动剂。它还是能够上调 CYP450 表达的孕烷 X 受体(PXR) 激活剂。
T37826	CAY10462 CAY10462,CTK8E8405	P450	Metabolism
	CAY10462 (CTK8E8405) 是一种有效的 20-HETE 合酶 CYP4A11 的选择性抑制剂，IC50 为 8.8 nM。 CAY10462 对 1A、1C 和 3A CYP450 酶的效力降低近 200 倍。
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。
T1540	Doxepin hydrochloride Toruan,Doxepin HCl,Aponal,Novoxapin,盐酸多塞平	P450; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
	Doxepin hydrochloride (Aponal) 是一种可口服的三环抗抑郁剂，是选择性组胺受体 H1拮抗剂。它也是 CYP450抑制剂，抑制 CYP450 2C19和 CYP450 1A2。
T11556	HET0016	Others	Others
	HET0016 is a potent and selective 20-HETE synthase inhibitor (IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis). HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angi
T14021	20-HETE 20-hydroxy Arachidonic Acid	Others	Others
	20-HETE (20-hydroxy Arachidonic Acid) is a CYP450 metabolite and a potent vasoconstrictor and it is an endogenous inhibitor of the large-conductance Ca2+-activated K+ channel in renal arterioles. 20-HETE increases NADPH oxidase, ROS, and NF-κB activity, a
T11847L	Liarozole R75251 dihydrochloride,利阿唑	P450; Retinoid Receptor	Metabolism
	Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物，是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA)，具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM)，导致组织维甲酸水平增加。
T14186	17-ODYA 17-十八炔酸,Alkynyl Stearic Acid	Others; PROTAC Linker	Others; PROTAC
	17-ODYA (Alkynyl Stearic Acid) 是 CYP450 ω-羟化酶抑制剂。它能够抑制与花生四烯酸孵育的大鼠肾皮质微粒体形成 20-HETE 、dihydroxyeicosatrienoic acids、epoxyeicosatrienoic acids。它可以改善异丙肾上腺素诱导的培养心肌细胞凋亡和坏死。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T14841	BVT948	Phosphatase; P450; Histone Methyltransferase	Chromatin/Epigenetic; Metabolism
	BVT948 是一种蛋白酪氨酸磷酸酶抑制剂，还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 同工型。
T16704	Quilseconazole VT-1129	Others	Others
	Quilseconazole is an effective, orally active fungal Cyp51 inhibitor. it also binds tightly to cryptococcal CYP51 but weakly inhibits humans CYP450 enzymes.
T11088	Doxepin D3 Hydrochloride	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Doxepin D3 Hydrochloride is a deuterium-labeled doxepin hydrochloride.Doxepin hydrochloride is an oral active tricyclic antidepressant used as a sedative.Doxepin hydrochloride is also an effective CYP450 inhibitor, significantly inhibiting CYP450 2C19 and
T25716L	Liarozole HCl R75251,Liarozole hydrochloride,R 75251,R-75251
	Liarozole HCl is a benzimidazole derivative with antineoplastic activity. As a retinoic acid metabolism blocking agent, liarozole inhibits CYP450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, leading to an increase in endogenous ATRA production,
T78154	CS640
	CS640是一种钙调蛋白依赖性激酶选择性抑制剂，对CaMK1D、CaMK1B、CaMK1A、CaMK1G、PIP5K1C、MEK5、RIPK4和MLK3的抑制作用的IC50值分别为0.08、0.03、0.001、0.001、11.2、0.025、5.69和2.75μM。此外，CS640对CYP450 2C9和CYP450 2C19的IC50值分别为6和10μM。
T37180	Avanafil metabolite M16
	Avanafil metabolite M16 is a major inactive metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M16 and avanafil metabolite M4 , as well as minor metabolites.
T35847	16(R)-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that...
T37234	(±)14(15)-EpETE
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoi...
T37238	(±)19(20)-EpDPA
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic...
T36145	12(R)-HETE
	Biosynthesis of 12(R)-HETE in invertebrates is via lipoxygenation of arachidonic acid . In mammals, 12(R)-HETE can be produced by 12(R)-LOs and also by CYP450 oxidation. The activity of 12(R)-HETE in mammals is predominantly proinflammatory. 12(R)-HETE exhibits dose-dependent leukocyte chemotaxis at concentrations as low as 100 nM, and lowers intraocular pressure in rabbits.
T37181	Avanafil metabolite M4 Avanafil metabolite M4
	Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil . Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 , as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.
T35848	16(S)-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 16-HETE is a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation that demonstrates stereospecific biological activity. 16(S)-HETE inhibits proximal tubule ATPase activity by as much as 60% at a concentration of 2 μM.
T37235	(±)16(17)-EpDPA (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex...
T11847	Liarozole dihydrochloride R75251 dihydrochloride	Others	Others
	Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
T37788	Resorufin benzyl ether
	Resorufin benzyl ether is a fluorometric probe that acts as a substrate for cytochrome P450 (CYP)3A4. It is typically used near its apparent Km value of 30 μM to screen the inhibition/activation potential of test compounds, to predict potential drug-drug interactions, or to monitor other CYP450 activities. Upon enzyme cleavage, resorufin benzyl ether generates a red fluorescent product (ex. 571 nm/em. 585 nm).
T35850	19(S)-HETE
	19-HETE is one of the major cytochrome P450 (CYP450) metabolites of arachidonic acid that is released from the kidney in response to angiotensin II. When formed by the CYP2E1 isoform, 19-HETE is composed of 70% and 30% of the (S) and (R) stereoisomers, respectively. Both 19(S)- and 19(R)-HETE are potent vasodilators of renal preglomerular vessels. 19(S)-HETE stimulates both renal sodium-potassium ATPase and volume absorption in the rabbit proximal straight tubule.
T35849	17(S)-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites.17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney.17(S)-HETE inhibits proximal tubule ATPase activity by as much as 70% at a concentration of 2 μM.
T37228	(±)8(9)-EpETE
	Eicosapentaenoic acid is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE , relaxes vascular and airway smooth muscle by activating large conductance Ca2+-activated K+ (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo. The biological actions and physiological effects of this epox...
T37241	(±)4(5)-EpDPA methyl ester
	(±)4(5)-EpDPA methyl ester is a derivative of (±)4(5)-EpDPA which is stable enough to ship and handle routinely. The active free acid can be regenerated from the methyl ester by careful base hydrolysis. (±)4(5)EpDPA is a CYP450 metabolite of DHA which can be further metabolized to the diol metabolite. There are no published reports on the biological activity of (±)4(5)-EpDPA methyl ester at this time.
T35467	(±)18-HETE
	(±)18-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid. When formed by the CYP2E1 isoform, 18-HETE is comprised 100% of the (R) isomer. 18(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, whereas 18(S)-HETE does not affect perfusion pressure. 18-HETE has negligible effects on ATPase activity. 18(R)-HETE at 1 μM completely blocks 20-HETE-induced vasoconstriction of renal arterioles.
T35523	(±)17-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)17-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. At a concentration of 2 μM the (S)-enantiomer of 17-HETE inhibits proximal tubule ATPase activity by as much as 70%, whereas the (R)-isomer is inactive.
T36216	19(R)-HETE
	19-HETE is one of the major cytochrome P450 (CYP450) metabolites of arachidonic acid that is released from the kidney in response to angiotensin II. When formed by the CYP2E1 isoform, 19-HETE is composed of 70% and 30% of the (S) and (R) stereoisomers, respectively. Both 19(S)- and 19(R)-HETE are potent vasodilators of renal preglomerular vessels. However, 19(R)-HETE at 1 μM completely blocks 20-HETE-induced vasoconstriction of renal arterioles, whereas 19(S)-HETE remains inactive.
T37708	17(R)-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. 17-HETE is a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. 17(R)-HETE is an inactive isomer of 17-HETE, whereas the (S) enantiomer can inhibit proximal tubule ATPase activity at a concentration of 2 μM.
T73898	Paritaprevir dihydrate
	Paritaprevir (ABT-450) dihydrate，一种口服非结构蛋白3/4A (NS3/4A) 蛋白酶抑制剂，对HCV1a 和 1b 具有高效抗病毒活性，EC50值分别为1 nM 和 0.21 nM。此外，其作为SARS-CoV3CLpro 抑制剂，IC50为1.31 μM。其主要通过细胞色素P450 (CYP) 3A代谢，且利托那韦 (Ritonavir，CYP450 抑制剂) 能增强其血浆浓度和延长半衰期。
T35465	(±)16-HETE
	Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)16-HETE is the racemic version of a minor CYP450 metabolite of arachidonic acid released by the kidney upon angiotensin II stimulation. The biological activity of 16-HETE is stereospecific. 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney, however 16(S)-HETE does not affect perfusion pressure. At a concentration of 2 μM the (S)-enantiomer of 16-HETE inhibits pro...
T35715	N-desmethyl Eletriptan
	N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoproteinDrug Metab. Dispos.31(7)861-869(2003)
T35494	(±)11(12)-EET
	(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in t...
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。

化合物

Levobupivacaine

Cat.No: T1787

Target: Sodium Channel

Cat.No: T22394

Synonym: ABT450,ABT-450,帕利普韦,Veruprevir

Target: HCV Protease

Levobupivacaine hydrochloride

Cat.No: T6566

Synonym: Levobupivacaine HCl,(S)-(-)-Bupivacaine HCl,盐酸左布比卡因,(S)-(-)-Bupivacaine monohydrochloride

Target: Sodium Channel

2,3-dihydrothieno-Thiadiazole Carboxylate

Cat.No: T22003

Target: P450

1-Phenylpyrrole

Cat.No: T20373

Synonym: NSC16581,NSC-16581,1-苯基吡咯,NSC 16581

Target: Others

Isoetharine mesylate salt

Cat.No: T4983

Synonym: Isoetarine mesilate,异丙肾上腺素甲磺酸盐

Target: Others, Adrenergic Receptor

Cat.No: T37826

Synonym: CAY10462,CTK8E8405

Target: P450

Cat.No: T4567

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

Target: P450, Antibacterial

Doxepin hydrochloride

Cat.No: T1540

Synonym: Toruan,Doxepin HCl,Aponal,Novoxapin,盐酸多塞平

Target: P450, Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor

Cat.No: T11556

Target: Others

Cat.No: T14021

Synonym: 20-hydroxy Arachidonic Acid

Target: Others

Cat.No: T11847L

Synonym: R75251 dihydrochloride,利阿唑

Target: P450, Retinoid Receptor

Cat.No: T14186

Synonym: 17-十八炔酸,Alkynyl Stearic Acid

Target: Others, PROTAC Linker

Cat.No: T36696

Cat.No: T14841

Target: Phosphatase, P450, Histone Methyltransferase

Cat.No: T16704

Synonym: VT-1129

Target: Others

Doxepin D3 Hydrochloride

Cat.No: T11088

Target: Histamine Receptor

Cat.No: T25716L

Synonym: R75251,Liarozole hydrochloride,R 75251,R-75251

Cat.No: T78154

Avanafil metabolite M16

Cat.No: T37180

Cat.No: T35847

(±)14(15)-EpETE

Cat.No: T37234

(±)19(20)-EpDPA

Cat.No: T37238

Cat.No: T36145

Avanafil metabolite M4

Cat.No: T37181

Synonym: Avanafil metabolite M4

Cat.No: T35848

(±)16(17)-EpDPA

Cat.No: T37235

Synonym: (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA

Liarozole dihydrochloride

Cat.No: T11847

Synonym: R75251 dihydrochloride

Target: Others

Resorufin benzyl ether

Cat.No: T37788

Cat.No: T35850

Cat.No: T35849

Cat.No: T37228

(±)4(5)-EpDPA methyl ester

Cat.No: T37241

Cat.No: T35467

Cat.No: T35523

Cat.No: T36216

Cat.No: T37708

Paritaprevir dihydrate

Cat.No: T73898

Cat.No: T35465

N-desmethyl Eletriptan

Cat.No: T35715

Cat.No: T35494

Cat.No: T79568

Target: Parasite

Cat. No.	Product Name	Target	Signaling Pathways
T2S0663	Humantenmine	P450	Metabolism
	Humantenmine 是一种分离自中国线虫中的生物碱，有用于疼痛和风湿性关节炎的研究潜力。
T3696	polygalaxanthone III	Others; P450	Metabolism; Others
	Polygalaxanthone III 提取自远志polygala tenuifolia wild，可抑制CYP450酶。它能够抑制由 CYP2E1 催化的氯唑沙宗 6-羟基化(IC50:50.56μM)。
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。

天然产物

Cat.No: T2S0663

Target: P450

polygalaxanthone III

Cat.No: T3696

Target: Others, P450

TETRAHYDROPIPERINE

Cat.No: T5786

Synonym: 四氢胡椒碱,Cosmoperine

Target: P450, TRP/TRPV Channel

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