HX-1171(HX-1171) - 药物靶点：Nrf2_专利_临床

概要

基本信息

药物类型

小分子化药

别名

HTHQ

靶点

Nrf2

作用机制

Nrf2刺激剂(核转录因子的激活红细胞2相关因子刺激剂)

治疗领域

消化系统疾病肿瘤免疫系统疾病+ [2]

在研适应症-

非在研适应症

动脉粥样硬化溃疡性结肠炎肝硬化+ [3]

原研机构

Nippon Hypox Laboratories Inc.

在研机构-

非在研机构

Biotoxtech Co., Ltd.Nippon Hypox Laboratories Inc.

最高研发阶段终止临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C15H24O2

InChIKeyATMNQRRJNBCQJO-UHFFFAOYSA-N

CAS号148081-72-5

关联

2

项与 HX-1171 相关的临床试验

NCT01889745 / Temporarily not availableN/A

A Phase I Clinical Study, Randomized, Single-blind,Placebo-controlled, Multiple Doses, Dose Escalation Study fo the Safety, Tolerability and Pharmacokinetics of HX-1171 in Healthy Male Subjects.

This study is designed to multiple dose and dose escalation study

开始日期-

申办/合作机构

Biotoxtech Co., Ltd.

NCT01548391 / Unknown status临床1期

A Phase I Clinical Study Study of the Safety, Tolerability, and Pharmacokinetics of HX-1171 in Healthy Male Subjects

This study is designed to evaluate the safety, tolerability, and pharmacokinetics of HX-1171 in healthy male subjects.

开始日期2012-03-01

申办/合作机构

Biotoxtech Co., Ltd.

100 项与 HX-1171 相关的临床结果

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100 项与 HX-1171 相关的转化医学

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100 项与 HX-1171 相关的专利（医药）

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26

项与 HX-1171 相关的文献（医药）

2024-05-01·Neurochemical Research

6-Hydroxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline Demonstrates Neuroprotective Properties in Experimental Parkinson's Disease by Enhancing the Antioxidant System, Normalising Chaperone Activity and Suppressing Apoptosis

Article

作者: Shikhaliev, Khidmet S ; Oleinik, Sergei A ; Medvedeva, Svetlana M ; Popova, Tatyana N ; Razuvaev, Grigorii A ; Kryl'skii, Evgenii D

Parkinson's disease (PD) is a neurodegenerative disease, whereby disturbances within the antioxidant defence system, increased aggregation of proteins, and activation of neuronal apoptosis all have a crucial role in the pathogenesis. In this context, exploring the neuroprotective capabilities of compounds that sustain the effectiveness of cellular defence systems in neurodegenerative disorders is worthwhile. During this study, we assessed how 6-hydroxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline (HTHQ), which has antioxidant properties, affects the functioning of the antioxidant system, the activity of NADPH-generating enzymes and chaperones, and the level of apoptotic processes in rats with rotenone-induced PD. Six groups of animals were formed for our experiment, each with 12 animals. These were: a control group, animals with rotenone-induced PD, rats with PD given HTHQ at a dose of 50 mg/kg, rats with PD given HTHQ at a dose of 25 mg/kg, animals with pathology who were administered a comparison drug rasagiline, and control animals who were administered HTHQ at a dose of 50 mg/kg. The study results indicate that administering HTHQ led to a significant decrease in oxidative stress in PD rats. The enhanced redox status in animal tissues was linked with the recovery of antioxidant enzyme activities and NADPH-generating enzyme function, as well as an upsurge in the mRNA expression levels of antioxidant genes and factors Nrf2 and Foxo1. Administering HTHQ to rats with PD normalized the chaperone-like activity and mRNA levels of heat shock protein 70. Rats treated with the compound displayed lower apoptosis intensity when compared to animals with pathology. Therefore, owing to its antioxidant properties, HTHQ demonstrated a beneficial impact on the antioxidant system, resulting in decreased requirements for chaperone activation and the inhibition of apoptosis processes triggered in PD. HTHQ at a dose of 50 mg/kg had a greater impact on the majority of the examined variables compared to rasagiline.

2023-09-21·Current issues in molecular biology

6-Hydroxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline Alleviates Oxidative Stress and NF-κB-Mediated Inflammation in Rats with Experimental Parkinson's Disease.

Article

作者: Popova, Tatyana N ; Medvedeva, Svetlana M ; Razuvaev, Grigorii A ; Shikhaliev, Khidmet S ; Kryl'skii, Evgenii D

A study was conducted to investigate the effects of different doses of 6-hydroxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline (HTHQ) on motor coordination scores, brain tissue morphology, the expression of tyrosine hydroxylase, the severity of oxidative stress parameters, the levels of the p65 subunit of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) factor, and the inflammatory response in rats during the development of rotenone-induced Parkinsonism. The findings indicate that HTHQ, with its antioxidant attributes, reduced the levels of 8-isoprostane, lipid oxidation products, and protein oxidation products. The decrease in oxidative stress due to HTHQ led to a reduction in the mRNA content of proinflammatory cytokines and myeloperoxidase activity, accompanying the drop in the expression of the factor NF-κB. These alterations promoted an improvement in motor coordination scores and increased tyrosine hydroxylase levels, whereas histopathological changes in the brain tissue of the experimental animals were attenuated. HTHQ exhibited greater effectiveness than the comparative drug rasagiline based on the majority of variables.

2021-01-01·Oxidative Medicine and Cellular Longevity2区 · 生物学

1‐O‐Hexyl‐2,3,5‐Trimethylhydroquinone Ameliorates the Development of Preeclampsia through Suppression of Oxidative Stress and Endothelial Cell Apoptosis

2区 · 生物学

ArticleOA

作者: Ma, Yuyan ; Gao, Na ; Jiang, Lai ; Yang, Qiuhong ; Li, Guiyang ; Gong, Yanping ; Rao, Jie

1‐O‐Hexyl‐2,3,5‐trimethylhydroquinone (HTHQ), a potent nuclear factor‐E2‐related factor 2 (Nrf2) activator, has potent antioxidant activity by scavenging reactive oxygen species (ROS). However, the role of HTHQ on the development of preeclampsia (PE) and the underlying mechanisms have barely been explored. In the present study, PE model was induced by adenovirus‐mediated overexpression of soluble fms‐like tyrosine kinase 1 (sFlt‐1) in pregnant mice. The results showed that HTHQ treatment significantly relieved the high systolic blood pressure (SBP) and proteinuria and increased the fetal weight and fetal weight/placenta weight in preeclamptic mice. Furthermore, we found that HTHQ treatment significantly decreased soluble endoglin (sEng), endothelin‐1 (ET‐1), and activin A and restored vascular endothelial growth factor (VEGF) in preeclamptic mice. In addition, HTHQ treatment inhibited oxidative stress and endothelial cell apoptosis by increasing the levels of Nrf2 and its downstream haemoxygenase‐1 (HO‐1) protein. In line with the data in vivo, we discovered that HTHQ treatment attenuated oxidative stress and cell apoptosis in human umbilical vein endothelial cells (HUVECs) following hypoxia and reperfusion (H/R), and the HTHQ‐mediated protection was lost after transfected with siNrf2. In conclusion, these results suggested that HTHQ ameliorates the development of preeclampsia through suppression of oxidative stress and endothelial cell apoptosis.

100 项与 HX-1171 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB12162

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
动脉粥样硬化	临床1期	韩国	-	-
溃疡性结肠炎	临床1期	韩国	-	-
肝硬化	临床1期	-	Biotoxtech Co., Ltd.	-
肝硬化	临床1期	-	Nippon Hypox Laboratories Inc.	-
肝病	临床1期	韩国	-	-
肿瘤	临床1期	日本	Nippon Hypox Laboratories Inc.	-
系统性红斑狼疮	临床1期	韩国	-	-