42
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T63337 | CYP2C19-IN-1 | ||
CYP2C19-IN-1 是强效的,无遗传毒性的、无肝脏毒性的 CYP2C19 抑制剂。 CYP2C19-IN-1 能够抑制 RNA 依赖的 RNA 聚合酶 (RdRP) (Ki: 6.16 μM),能够用于研究寨卡病毒 (ZIKV) 感染。 | |||
T63495 | CYP2C1/CYP2C19-IN-2 | ||
CYP2C1/CYP2C19-IN-2 是无肝脏毒性和遗传毒性的CYP2C9/CYP2C19强效抑制剂,能够用于研究寨卡病毒 (ZIKV) 感染。 | |||
T21529 |
(S)-Mephenytoin
|
Others | Others |
(S)-Mephenytoin 是一种抗惊厥剂。(S)-Mephenytoin 作为细胞色素 P450 (CYP) 同种型 CYP2C19 的底物,可用于分析细胞色素 P450 代谢。 | |||
T63496 | CYP2C9/CYP2C19-IN-1 | ||
CYP2C9/CYP2C19-IN-1 是无肝脏毒性和遗传毒性的CYP2C9/CYP2C19强效抑制剂,能够用于研究寨卡病毒 (ZIKV) 感染。 | |||
T21425 |
Mephenytoin
Mesantoin,Methoin,Insulton,Phenantoin,美芬妥因,Methylphenetoin |
P450 | Metabolism |
Mephenytoin (Phenantoin) 是 CYP2C19 及 CYP2B6 的底物,是一种抗惊厥剂。 | |||
T3610 |
Ranitidine
雷尼替丁,HSDB 3925,Ranitidin |
P450; Antibacterial; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience |
Ranitidine (HSDB 3925) 是一种选择性的,具有口服活性的组胺 H2 受体拮抗剂,IC50为 3.3 μM。它还一种是CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。 | |||
T0865 |
Ranitidine Hydrochloride
AH19065,盐酸雷尼替丁 |
P450; Antibacterial; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience |
Ranitidine Hydrochloride (AH19065) 是一种具有口服活性的组胺 H2 受体选择性拮抗剂,IC50为 3.3 μM。它还是一种CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。 | |||
T4190 |
Ticlopidine
PCR 5332,Ticlid,噻氯匹定 |
ATPase; Adiponectin receptor | GPCR/G Protein; Membrane transporter/Ion channel |
Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。 | |||
T21029 |
Norfluoxetine Hydrochloride
Norfluoxetine HCl,去甲氟西汀 |
Others | Others |
Norfluoxetine Hydrochloride (Norfluoxetine HCl) 是氟西汀的活性代谢物。氟西汀是一种抗抑郁药。 | |||
T0182L |
Clopidogrel hydrogen sulfate
硫酸氢氯吡格雷,(S)-(+)-Clopidogrel hydrogen sulfate,(S)-(+)-Clopidogrel bisulfate,SR-25990C,Clopidogrel,硫酸氯吡格雷 |
P450; P2Y Receptor | GPCR/G Protein; Metabolism; Neuroscience |
Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) 是一种抗血小板药物,可防止血栓形成。它抑制 CYP2B6和 CYP2C19,IC50分别为 18.2 和 524 nM。 它是一种选择性的高亲和力 P2Y12 受体拮抗剂,可抑制纤维蛋白原与血小板的结合以及血小板的粘附和聚集。 | |||
T67926 |
(S)-(+)-N-3-Benzylnirvanol
ZSN-76403 |
P450; HIV Protease | Metabolism; Microbiology/Virology; Proteases/Proteasome |
(S)-(+)-N-3-Benzylnirvanol (ZSN-76403) 是一种细胞色素P450 CYP2C19抑制剂,IC50值为0.179 µM,可用于研究艾滋病毒感染。 | |||
T4498 |
Stiripentol
斯利潘托,BCX2600,Diacomit |
P450 | Metabolism |
Stiripentol (BCX2600) 是抗惊厥剂,对 CYP3A4 (非竞争性) 及 CYP2C19 (竞争性地) 介导的 CLB 向 N-desmethylclobazam (NCLB) 的 N-去甲基化具有抑制作用。 | |||
T37332 |
(±)-N-3-Benzylnirvanol
|
P450 | Metabolism |
(±)-N-3-Benzylnirvanol 是由(+)-N-3-Benzylnirvanol 和 (-)-N-3-Benzylnirvanoll 混装在一起的外消旋混合物。(+)-N-3-Benzylnirvanol 和 (-)-N-3-Benzylnirvanoll 是细胞色素 P450的选择性抑制剂,对 CYP2C19具有抑制作用,(±)- n -3-苄基壬烷醇可降低小鼠血浆胆固醇水平。 | |||
T9335 |
1,1'-Methylenedi-2-naphthol
1,1-亚甲基-2-萘酚,Squoxin |
Others | Others |
1,1'-Methylenedi-2-naphthol 靶向 CYP2C19 - 细胞色素 P450 家族 2 亚家族 C 成员 19(人)。 | |||
T22391 |
Omeprazole Sodium
|
P450; Proton pump; Antibacterial; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology |
Omeprazole 是有效的质子泵抑制剂,在胃肠道疾病的研究中具有价值。它竞争性抑制CYP2C19活性,Ki 为 2 到 6 μM。它还抑制革兰氏阴性菌和革兰氏阳性菌生长。它是中性鞘磷脂酶的外泌体抑制剂。 | |||
T10138 |
4-Desmethoxy Omeprazole
|
Drug Metabolite | Metabolism |
4-Desmethoxy Omeprazole 是 Omeprazole 的活性代谢物。Omeprazole 是质子泵抑制剂。Omeprazole 竞争性抑制 CYP2C19 活性,Ki=2 - 6 μM。Omeprazole 还抑制革兰氏阴性菌和革兰氏阳性菌生长。 | |||
T20570 |
Labetalol
Apo-Labetalol,Albetol,Trandate,Dilevalol,拉贝洛尔,Normodyne |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Labetalol (Apo-Labetalol) 是一种抗高血压药物,可用于心血管疾病的研究,如妊娠期高血压。它是一种口服具有活性的选择性 α1- 和非选择性 β-肾上腺素能受体 (adrenergic receptor) 竞争性拮抗剂。 | |||
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。 | |||
T0757 |
Omeprazole
Losec,Prilosec,奥美拉唑,奥美拉挫,H 16868,Antra |
Proton pump; Phospholipase; Antibacterial; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology |
Omeprazole (Losec) 是一种质子泵抑制剂,有研究胃肠道疾病的潜力。它竞争性抑制 CYP2C19活性,Ki 为 2 到 6 μM。它还抑制革兰氏阳性菌和革兰氏阴性菌生长。它是中性鞘磷脂酶的外泌体抑制剂。 | |||
T1149 |
Fenofibrate
Procetofen,非诺贝特,Lipanthyl,Lipantil |
P450; PPAR; Autophagy | Autophagy; DNA Damage/DNA Repair; Metabolism |
Fenofibrate (Lipanthyl) 是一种选择性PPARα激动剂,EC50为 30 μM。它是一种合成的苯氧基异丁酸衍生物和前药,具有抗高血脂活性。它抑制细胞色素 P450 亚型, 对CYP2C19、CYP2B6、CYP2C9、CYP2C8和CYP3A4的IC50分别为 0.2、0.7、9.7、4.8 和 142.1 μM。 | |||
T6249 |
Avagacestat
BMS-708163 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
Avagacestat (BMS-708163) 是一种有效的γ-secretase 抑制剂,抑制 Aβ42 (IC50:0.27 nM) 和 Aβ40 (IC50:0.30 nM) 的产生。它同时抑制 Notch 胞内结构域 (NICD) (IC50:0.84 nM) 和 CYP2C19 (IC50:20 nM) 。它可用于阿尔兹海默症的研究。 | |||
T23586 |
5-Hydroxylansoprazole sulfone
AG1909,AG 1909,AG-1909 |
||
5-hydroxylansoprazole is an in vitro metabolism-dependent CYP2C19 inhibitor. | |||
T36530 | Pantoprazole sulfone | ||
Pantoprazole sulfone is a metabolite of the gastric H+/K+ ATPase pump inhibitor pantoprazole . Pantoprazole is metabolized by the cytochrome P450 (CYP) isoforms CYP2C19 and CYP3A4 to form pantoprazole sulfone. | |||
T37796 |
Voriconazole N-oxide
|
||
Voriconazole N-oxide is a major metabolite of the triazole antifungal voriconazole . It is formed via oxidation of voriconazole by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19. | |||
T35431 |
(±)-Clopidogrel (hydrochloride)
|
||
Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix , clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascu... | |||
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。 | |||
T37247 |
Pantoprazole Sulfide
|
||
Pantoprazole sulfide is a metabolite of the gastric H+/K+ ATPase pump inhibitor pantoprazole . Pantoprazole is metabolized by the cytochrome P450 (CYP) isomers CYP2C19 and CYP3A4 to form pantoprazole sulfide. | |||
T14051 |
5-Hydroxylansoprazole
AG1908 |
Proton pump | Membrane transporter/Ion channel |
5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole, a gastric proton-pump inhibitor that effectively treats various peptic diseases[1][2]. The metabolism of Lansoprazole occurs through CYP2C19, resulting in the formation of 5-Hydroxylansoprazole. | |||
T36112 |
Clopidogrel Carboxylic Acid (hydrochloride)
|
||
Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active thiol metabolite via CYP2C19 in the liver enables its anti-aggregating activity. An estimated 15% of administered clopidogrel is metabolized by CYP2C19 to the thiol metabolite. Clopidogrel carboxylic acid i... | |||
T35718 |
N-desmethyl Rosuvastatin (sodium salt hydrate)
|
||
N-desmethyl Rosuvastatin is an active metabolite of the HMG-CoA reductase inhibitor rosuvastatin .1,2N-desmethyl Rosuvastatin is formed when rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.1 1.Macwan, J.S., Ionita, I.A., and Akhlaghi, F.A simple assay for the simultaneous determination of rosuvastatin acid, rosuvastatin-5S-lactone, and N-desmethyl rosuvastatin in human plasma using liquid chromatography-tand... | |||
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。 | |||
T36840 |
(R)-Omeprazole (sodium salt)
|
||
(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxidation of the active (S)-enantiomer . (R)-Omeprazole has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes (IC50 = 8.1 μM). | |||
T37659 |
5-hydroxy Omeprazole
|
||
5-hydroxy Omeprazole is a major metabolite of omeprazole , an inhibitor of the gastric H+/K+-ATPase pump.[1] 5-hydroxy Omeprazole is produced from omeprazole by the action of cytochrome P450 (CYP) isoform 2C19, a monooxygenase. [2][3] CYP2C19 polymorphisms significantly influence the metabolism of omeprazole, and individuals may be classified as homozygous extensive metabolizers, heterozygous extensive metabolizers, and poor metabolizers.[1] | |||
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... | |||
T78590 |
Dibenzylfluorescein
DBF |
||
Dibenzylfluorescein(DBF)是一款荧光探针,作为细胞色素P450(CYP)亚型,包括CYP3A4、CYP2C8、CYP2C9、CYP2C19和CYP19的特异性底物,常在Km值0.87-1.9 µM(Ex=485nm,Em=535nm)范围内应用。该探针主要用于监测药物或疾病导致的CYP催化活性变化。 | |||
T78925 |
HIV-1 inhibitor-58
|
||
HIV-1inhibitor-58(Compound 10c)是一款抗逆转录病毒活性的广谱非核苷逆转录酶抑制剂,有效抑制MT-4细胞中的HIV-1 WT株IIIB以及NNRTI耐药菌株,如K103N和E138K(EC50 < 50 nM)。此外,HIV-1inhibitor-58对CYP2C9与CYP2C19也表现出抑制作用(IC50分别为2.06 μM与1.91 μM),适用于HIV感染研究。 | |||
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 ... | |||
T62452 | HIV-1 inhibitor-40 | ||
HIV-1 inhibitor-40 (Compound 4ab) 是一种 HIV-1 非核苷型逆转录酶抑制剂 (NNRTI) (EC50: 1.9 nM),体内没有明显急性毒性。HIV-1 inhibitor-40 对 CYP 的敏感性较低,作用于 CYP2C9 (IC50: 5.16 μM) 和 CYP2C19 (IC50: 4.51 μM)。 | |||
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。 | |||
T35829 | CC-90005 | ||
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS... | |||
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. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10147 |
4-Hydroxymephenytoin
(+/-)-4'-Hydroxymephenytoin |
Others; Drug Metabolite | Metabolism; Others |
4-Hydroxymephenytoin ((+/-)-4'-Hydroxymephenytoin) 是抗癫痫药 mephenytoin 的代谢产物。Mephenytoin 是 CYP2C19的配体。 | |||
T3818 |
Fraxinol
|
Others; P450 | Metabolism; Others |
Fraxinol 是一种分离自半边莲中的化合物。 | |||
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。 | |||
T5S2360 |
Corydaline
Corydalin,紫堇碱,延胡索甲素,(+)-Corydaline |
P450; Virus Protease; Opioid Receptor; AChE | Endocrinology/Hormones; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience |
Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱,是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运,促进胃的调节,具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。 | |||
TN1378 |
α-Viniferin
ALPHA-VINIFERIN,Alpha-葡萄素 |
P450; NO Synthase; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism |
α-Viniferin 也称为2-芳基苯并呋喃类黄酮,是前列腺素H2合成酶抑制剂。具有抗阿尔茨海默病、抗结核、抗肿瘤、抗炎、抗糖尿病等多种药理活性 |