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11

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T22003 2,3-dihydrothieno-Thiadiazole Carboxylate

P450 Metabolism
2,3-dihydrothieno-Thiadiazole Carboxylate 是一种 CYP450(CYP2E1CYP2B4)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

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

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

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

(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

(±)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

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

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。

化合物

2,3-dihydrothieno-Thiadiazole Carboxylate
Cat.No: T22003
Synonym:
Target: P450
Clomethiazole
Cat.No: T14983
Synonym: Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE
Target: P450, GABA Receptor
Fomepizole
Cat.No: T0765
Synonym: Antizol-Vet,4-甲基吡唑,甲吡唑,4-Methylpyrazole,Antizol
Target: P450, CAT, AChR
GYKI-47261 dihydrochloride
Cat.No: T38601
Synonym:
Target:
6-hydroxy Chlorzoxazone
Cat.No: T37306
Synonym: 6-hydroxy Chlorzoxazone,NSC 24955
Target:
Fomepizole hydrochloride
Cat.No: T72245
Synonym: 4-Methylpyrazole hydrochloride
Target:
(3S)-hydroxy Quinidine
Cat.No: T36561
Synonym:
Target:
(±)18-HETE
Cat.No: T35467
Synonym:
Target:
19(S)-HETE
Cat.No: T35850
Synonym:
Target:
19(R)-HETE
Cat.No: T36216
Synonym:
Target:
2-Phenyl-2-(1-piperidinyl)propane
Cat.No: T7788
Synonym:
Target: Others
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。

天然产物

Schisandrol B
Cat.No: T6S1917
Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B
Target: P450, Reactive Oxygen Species, Autophagy
polygalaxanthone III
Cat.No: T3696
Synonym:
Target: Others, P450
ε-​Viniferin
Cat.No: T11218
Synonym: epsilon-Viniferin,Epsilon-白藜芦醇脱氢二聚体
Target: P450
Tenuifoliside C
Cat.No: T2S2211
Synonym:
Target: Dehydrogenase
Friedelin
Cat.No: TN1650
Synonym: 软木三萜酮,无羁萜
Target: P450, NOS, Caspase, Prostaglandin Receptor
Fraxinol
Cat.No: T3818
Synonym:
Target: Others, P450
Eleutheroside E
Cat.No: T3662
Synonym:
Target: NF-κB
Demethyleneberberine
Cat.No: T4S0800
Synonym:
Target: P450, NOS, NF-κB, HIF, AMPK
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