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21

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T20215 Acetaminophen mercapturate

Paracetamol Mercapturate is a metabolite of Acetaminophen. It can also be used in the biological study of urinary antihypertensive drugs.
T19175 Acetaminophen metabolite 3-hydroxy-acetaminophen

对乙酰氨基酚代谢物,3-Hydroxyacetaminophen

Others Others
3-hydroxy-acetaminophen is a metabolite of Acetaminophen. Acetaminophen is a pain medicine.
T36826 Acetaminophen Glucuronide (sodium salt)

Acetaminophen glucuronide is an inactive metabolite of the analgesic and antipyretic agent acetaminophen . It is formed via glucuronidation of acetaminophen by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A6, UGT1A9, UGT1A1, and UGT2B15.
T38206 3-Cysteinylacetaminophen (trifluoroacetate salt)

APAP-Cys,3-(cysteine-S-yl)acetaminophen,3-Cysteinylacetaminophen (trifluoroacetate salt)

3-Cysteinylacetaminophen is an acetaminophen-protein adduct formed during the metabolism of acetaminophen.[1],[2] 3-Cysteinylacetaminophen has been found in isolated human serum following therapeutic and supratherapeutic doses of acetaminophen and in the presence and absence of hepatotoxicity.[3],[4] In mice, 3-cysteinylacetaminophen decreases renal glutathione (GSH) levels, an effect that can be blocked by the γ-glutamyl inhibitor acivicin.
T29415 3-Methylacetaminophen

3-Methylacetaminophen is a bioactive chemical.
T4545 Propacetamol Hydrochloride

盐酸丙帕他莫,Propacetamol HCL

Others Others
Propacetamol Hydrochloride (Propacetamol HCL) 是 paracetamol(acetaminophen) 的前药,具有改善的水溶性。当口服非甾体抗炎药不合适或矛盾时,丙帕西莫是一种静脉给药的镇痛药。
T0914 Metacetamol

酰胺苯酚,3-Acetamidophenol

Others Others
Metacetamol (3-Acetamidophenol) 是对乙酰氨基酚的衍生物,为其无毒区域异构体,是一种非处方镇痛剂和解热剂,也可用作有机合成中间体。
T7280 CAY10594

Phospholipase Metabolism
CAY10594 是磷脂酶 D2 抑制剂 (体外IC50=140 nM,细胞IC50=110 nM)。它在体外显著阻碍乳腺癌细胞的侵袭性迁移,并调节磷酸化 GSK-3β/JNK 轴改善扑热息痛诱导的急性肝损伤。
TF0106 Cholesteryl Hemisuccinate Tris Salt

Apoptosis Apoptosis
Cholesteryl Hemisuccinate Tris Salt 是一种具有保肝和抗癌活性的酸性胆固醇酯,是一种含有柴胡皂苷-d的二棕榈酰磷脂酰胆碱脂质体中的膜稳定剂,可增强顺铂的抗癌功效。Cholesteryl hemisuccinate 具有抗肿瘤活性,抑制肿瘤生长,抑制对乙酰氨基酚 (AAP) 的肝毒性,预防 AAP 诱导的肝细胞凋亡。Cholesteryl hemisuccinate 可保护啮齿动物免受对乙酰氨基酚、阿霉素、四氯化碳、氯仿和半乳糖胺的毒性作用。
T67509 Cholesteryl Hemisuccinate

Cholesterol hydrogen succinate

Apoptosis; DNA/RNA Synthesis; Topoisomerase Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) 是一种经常使用在极性溶液中具有高溶解度的胆固醇类似物 ,具有保肝、抗癌和抑制肿瘤生长的作用。Cholesteryl Hemisuccinate 抑制对乙酰氨基酚 的肝毒性,并防止 AAP 诱导的肝细胞凋亡 和坏死 。Cholesteryl Hemisuccinate 抑制 DNA 聚合酶 和 DNA 拓扑异构酶 ,从而抑制 DNA 复制和修复以及细胞分裂。
T9948 NecroX-7

LC-280126,LC28-0126,LC28 0126

NADPH-oxidase Immunology/Inflammation
NecroX-7 (LC-280126) 是一种有效的自由基清除剂和 HMGB1(高迁移率族蛋白 1) 抑制剂。NecroX-7 可以作为对乙酰氨基酚毒性的解毒剂。NecroX-7 通过抑制缺血/再灌注损伤中 HMGB1 的释放发挥保护作用。NecroX-7 抑制 HMGB1 诱导的 TNF 和 IL-6的释放,以及TLR-4和晚期糖基化终产物受体的表达,用于移植物抗宿主病 (GVHD) 研究。
T33881 Paracetamol mercapturate

Paracetamol mercapturate is a deuterated metabolite of acetaminophen.
T10135 4-Acetamidophenyl acetate

Others Others
4-Acetamidophenyl acetate is an impurity of Acetaminophen. Acetaminophen is a selective COX-2 inhibitor (IC50: 25.8 μM) and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
T10143 4-Hydroxyacetophenone oxime

Others Others
4-Hydroxyacetophenone oxime is an impurity of Acetaminophen (Paracetamol). Acetaminophen is a potent COX-2 and hepatic NAT2 inhibitor and used antipyretic and analgesic drug.
T69218 PUMAi HCl

PUMAi is an inhibitor of p53 up-regulated modulator of apoptosis (PUMA), a BH3-only Bcl-2 family member, mitigating acetaminophen (APAP)-induced hepatocyte necrosis and liver injury.
T83050 Anti-inflammatory agent 62

Anti-inflammatory agent 62 减轻乙酰氨基酚诱导的HepG2肝毒性,其机制是通过调节炎症和氧化应激途径。
T38312 L-Cysteine-glutathione disulfide

L-Cysteine-glutathione disulfide, a glutathione derivative endogenous to mammalian cells, is comprised of the oxidized form of free glutathione tripeptide linked via a disulfide bond to L-cysteine. It has been shown to protect mice against acetaminophen-induced hepatotoxicity.
T11752 Keap1-Nrf2-IN-1

Keap1–Nrf2-IN-1

Src Angiogenesis; Tyrosine Kinase/Adaptors
Keap1–Nrf2 IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models. Keap1–Nrf2 IN-1 is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (
T76364 Ac-Leu-Leu-Norleucinol

Ac-Leu-Leu-Norleucinol 是钙蛋白酶抑制剂,可用于研究对 Acetaminophen 引起的急性肝损伤,并能够降低诱导引发的谷草转氨酶 (ALT) 和谷丙转氨酶 (AST) 水平。
T64218 Keap1-Nrf2-IN-1 TFA

Keap1-Nrf2-IN-1 TFA (compound35) 是一种 Keap1-Nrf2 蛋白-蛋白相互作用抑制剂 (IC50: 43 nM),可以激活 Nrf2 调节的细胞保护反应。在细胞和体内模型中。Keap1-Nrf2-IN-1 TFA 能够拮抗对乙酰氨基酚诱导的肝损伤。
T63930 DI-1859

DI-1859 是选择性的、有效的、共价的 DCN1 抑制剂。低纳摩尔浓度下,DI-1859 能够抑制细胞中 cullin 3 的 neddylation。DI-1859 能够促使小鼠肝脏中 NRF2 蛋白(一种 CRL3 底物)显著提高,并有效保护小鼠,防止乙酰氨基酚诱导的肝损伤。

化合物

Acetaminophen mercapturate
Cat.No: T20215
Synonym:
Target:
Acetaminophen metabolite 3-hydroxy-acetaminophen
Cat.No: T19175
Synonym: 对乙酰氨基酚代谢物,3-Hydroxyacetaminophen
Target: Others
Acetaminophen Glucuronide (sodium salt)
Cat.No: T36826
Synonym:
Target:
3-Cysteinylacetaminophen (trifluoroacetate salt)
Cat.No: T38206
Synonym: APAP-Cys,3-(cysteine-S-yl)acetaminophen,3-Cysteinylacetaminophen (trifluoroacetate salt)
Target:
3-Methylacetaminophen
Cat.No: T29415
Synonym:
Target:
Propacetamol Hydrochloride
Cat.No: T4545
Synonym: 盐酸丙帕他莫,Propacetamol HCL
Target: Others
Metacetamol
Cat.No: T0914
Synonym: 酰胺苯酚,3-Acetamidophenol
Target: Others
CAY10594
Cat.No: T7280
Synonym:
Target: Phospholipase
Cholesteryl Hemisuccinate Tris Salt
Cat.No: TF0106
Synonym:
Target: Apoptosis
Cholesteryl Hemisuccinate
Cat.No: T67509
Synonym: Cholesterol hydrogen succinate
Target: Apoptosis, DNA/RNA Synthesis, Topoisomerase
NecroX-7
Cat.No: T9948
Synonym: LC-280126,LC28-0126,LC28 0126
Target: NADPH-oxidase
Paracetamol mercapturate
Cat.No: T33881
Synonym:
Target:
4-Acetamidophenyl acetate
Cat.No: T10135
Synonym:
Target: Others
4-Hydroxyacetophenone oxime
Cat.No: T10143
Synonym:
Target: Others
PUMAi HCl
Cat.No: T69218
Synonym:
Target:
Anti-inflammatory agent 62
Cat.No: T83050
Synonym:
Target:
L-Cysteine-glutathione disulfide
Cat.No: T38312
Synonym:
Target:
Keap1-Nrf2-IN-1
Cat.No: T11752
Synonym: Keap1–Nrf2-IN-1
Target: Src
Ac-Leu-Leu-Norleucinol
Cat.No: T76364
Synonym:
Target:
Keap1-Nrf2-IN-1 TFA
Cat.No: T64218
Synonym:
Target:
DI-1859
Cat.No: T63930
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0065 Acetaminophen

对乙酰氨基酚,醋氨酚,4-Acetamidophenol,4'-Hydroxyacetanilide,APAP,Paracetamol

COX; Endogenous Metabolite; Histone Acetyltransferase Chromatin/Epigenetic; Immunology/Inflammation; Metabolism; Neuroscience
Acetaminophen (APAP) 是一种 COX 抑制剂,抑制 COX-1 和 COX-2 (IC50=113.7/25.8 μM)。Acetaminophen 具有解热镇痛活性,以及较弱的抗炎活性。
TN7063 N-Acetaminophen

NSC 403155,N-Acetyldemecolcine,N-Methylcolchicine,N-甲基-秋水仙碱,N-Acetylcolchamine

Others Others
N-Acetaminophen (N-Methylcolchicine) 是秋水仙碱的甲基化形式。
T3913 Saikosaponin D

Estrogen Receptor/ERR; NF-κB; Antibacterial; STAT Endocrinology/Hormones; JAK/STAT signaling; Microbiology/Virology; NF-κB; Stem Cells
Saikosaponin D 是一种从柴胡中分离到的三萜皂苷类天然产物,具有抗炎,抗菌,抗肿瘤,抗过敏作用。它抑制 selectin,STAT3和 NF-kB 的活性,活化estrogen receptor-β。
T4322 2-Hydroxybutyric acid

α-Hydroxybutyric acid

Endogenous Metabolite Metabolism
2-Hydroxybutyric acid (α-Hydroxybutyric acid) 是蛋白质代谢的产物,是 2 型糖尿病和先兆子痫的生物标志物,是合成生物降解材料和各种化合物的重要中间体。2-Hydroxybutyric acid 可预防 acetaminophen (AP) 引起的肝损伤,可参与抗肿瘤抗生素和可生物降解的聚(2-羟基丁酸)阿齐诺菊酯家族的合成。
T82219 Heilaohuguosu F

Heilaohuguosu F (compound 6)为一类四氢呋喃木脂素,表现出轻度肝脏保护效果。该化合物对于APAP诱导的HepG2细胞所呈现的肝毒性具有微弱的防护作用。
T82365 Fulvotomentoside B

Fulvotomentoside B, 一种可从黄毛乳杆菌中分离的皂苷,对于CCl4、d-gal 和对乙酰氨基酚所致中毒小鼠具有显著的保护作用。在减低血清SGPT和GT水平以及减轻肝脏病理损伤方面表现出突出的效果。
TN4223 Homopterocarpin

Antifection Microbiology/Virology
Homopterocarpin and Pterocarpus extract offer gastroprotection against indomethacin- induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis, homopterocarpin may be responsible for, or contribute to the antiulcerogenic property

天然产物

Acetaminophen
Cat.No: T0065
Synonym: 对乙酰氨基酚,醋氨酚,4-Acetamidophenol,4'-Hydroxyacetanilide,APAP,Paracetamol
Target: COX, Endogenous Metabolite, Histone Acetyltransferase
N-Acetaminophen
Cat.No: TN7063
Synonym: NSC 403155,N-Acetyldemecolcine,N-Methylcolchicine,N-甲基-秋水仙碱,N-Acetylcolchamine
Target: Others
Saikosaponin D
Cat.No: T3913
Synonym:
Target: Estrogen Receptor/ERR, NF-κB, Antibacterial, STAT
2-Hydroxybutyric acid
Cat.No: T4322
Synonym: α-Hydroxybutyric acid
Target: Endogenous Metabolite
Heilaohuguosu F
Cat.No: T82219
Synonym:
Target:
Fulvotomentoside B
Cat.No: T82365
Synonym:
Target:
Homopterocarpin
Cat.No: TN4223
Synonym:
Target: Antifection
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