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Cat. No. | Product Name | Target | Signaling Pathways |
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T22003 |
2,3-dihydrothieno-Thiadiazole Carboxylate
|
P450 | Metabolism |
2,3-dihydrothieno-Thiadiazole Carboxylate 是一种 CYP450(CYP2E1 和 CYP2B4)抑制剂。 | |||
T14983 |
Clomethiazole
Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE |
P450; GABA Receptor | Membrane transporter/Ion channel; Metabolism; Neuroscience |
Clomethiazole (Distraneurin) 是口服GABAA 激动剂,可抑制人肝微粒体中的细胞色素 P450 异构体,CYP2A6 和 CYP2E1。它有抗惊厥作用,具有治疗惊厥性癫痫持续状态的潜力。 | |||
T0765 |
Fomepizole
Antizol-Vet,4-甲基吡唑,甲吡唑,4-Methylpyrazole,Antizol |
P450; CAT; AChR | Metabolism; Neuroscience; oxidation-reduction |
Fomepizole (4-Methylpyrazole) 是细胞色素 P450 (CYP2E1) 抑制剂。它是乙醇脱氢酶 (alcohol dehydrogenase) 竞争性抑制剂。它能够阻断甲醇和乙二醇进一步转化为有毒代谢产物。它具有成为乙二醇或甲醇中毒的解毒剂的潜力。 | |||
T38601 |
GYKI-47261 dihydrochloride
|
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GYKI-47261 dihydrochloride is a selective AMPA receptor antagonist, administered orally, and exhibits competitive activity with an IC 50 of 2.5 μM. It displays a wide range of anticonvulsive effects and demonstrates neuroprotective properties. Additionally, GYKI-47261 dihydrochloride is a potent inducer of CYP2E1. | |||
T37306 |
6-hydroxy Chlorzoxazone
6-hydroxy Chlorzoxazone,NSC 24955 |
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6-hydroxy Chlorzoxazone is a metabolite of chlorzoxazone. [1] It is formed by metabolism of chlorzoxazone by the cytochrome P450 (CYP) isoform CYP2E1 in human hepatic microsomes. | |||
T72245 |
Fomepizole hydrochloride
4-Methylpyrazole hydrochloride |
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Fomepizole hydrochloride(4-Methylpyrazole)是一种高效、具口服活性的细胞色素P450(CYP2E1)和竞争性乙醇脱氢酶(alcohol dehydrogenase)抑制剂,阻止甲醇和乙二醇转化为有毒代谢产物,具有用于乙二醇或甲醇中毒解毒的潜力。 | |||
T36561 |
(3S)-hydroxy Quinidine
|
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(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-depe... | |||
T35467 |
(±)18-HETE
|
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(±)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. | |||
T35850 |
19(S)-HETE
|
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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. | |||
T36216 |
19(R)-HETE
|
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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. | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 | |||
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)。 | |||
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。 | |||
T2S2211 |
Tenuifoliside C
|
Dehydrogenase | Metabolism |
Tenuifoliside C 是从野生的 polygala tenuifolia 中分离得到的。它对 CYP2E1 催化氯唑酮 6-羟基化反应具有抑制作用。 | |||
TN1650 |
Friedelin
软木三萜酮,无羁萜 |
P450; NOS; Caspase; Prostaglandin Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Metabolism; Proteases/Proteasome |
Friedelin 是分离自 Maytenus ilicifolia(Mart) 的叶子。它是 CYP3A4的非竞争性抑制剂,其 IC50和 Ki 分别为10.79 μM 和 6.16 μM,也是 CYP2E1的竞争性抑制剂,其 IC50和 Ki 分别为 22.54 μM 和 18.02 μM。 | |||
T3818 |
Fraxinol
|
Others; P450 | Metabolism; Others |
Fraxinol 是一种分离自半边莲中的化合物。 | |||
T3662 |
Eleutheroside E
|
NF-κB | NF-κB |
Eleutheroside E 是刺五加的重要成分,具有抗炎,保护缺血心脏的功能。 | |||
T4S0800 |
Demethyleneberberine
|
P450; NOS; NF-κB; HIF; AMPK | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling |
Demethyleneberberine 是从黄连中提取的一种天然产物,是线粒体靶向抗氧化剂。它也可作为AMPK 激活剂,用于非酒精性脂肪性肝病的研究。它通过抑制NF-κB 通路和调节 Th 细胞的平衡来减轻小鼠结肠炎并抑制炎症反应。 |