盐酸肼屈嗪 T1613

Product Introduction
Bioactivity


英文名: Hydralazine hydrochloride

描述: Hydralazine hydrochloride (Apresoline) 是一种直接作用的血管舒张剂，可抗高血压。

体外活性: Hydralazine impairs up-regulation of RAG-2 gene expression and reduces secondary Ig gene rearrangements. Hydralazine subverts B lymphocyte tolerance to self and contributes to generation of pathogenic autoreactivity by disrupting receptor editing. [1] Hydralazine directly scavenges free acrolein, decreasing intracellular acrolein availability and thereby suppressing macromolecular adduction. Hydralazine inhibits cross-linking if adding 30 min after commencing acrolein exposure but is ineffective if added after a 90-min delay. [2] Hydralazine (0.1-10 mM) inhibits both extracellular and intracellular ROS production by inflammatory macrophages, by a ROS-scavenging mechanism probably affecting superoxide radical (O(2)(*-))-generation by xanthine oxidase (XO) and nicotinamide adenine dinucleotide/nicotinamide adenine dinucleotide phosphate (NADH/NADPH) oxidase. Hydralazine (0.1-10 mM) significantly reduces NO(*) generation, and this effect is attributable to an inhibition of NOS-2 gene expression and protein synthesis. Hydralazine also effectively blocks COX-2 gene expression which perfectly correlated with a reduction of protein levels and PGE(2) synthesis. [3] Hydralazine protects against not only acrolein-mediated injury, but also compression in guinea pig spinal cord ex vivo. Hydralazine can significantly alleviate acrolein-induced superoxide production, glutathione depletion, mitochondrial dysfunction, loss of membrane integrity, and reduces compound action potential conduction. [4]

体内活性: Hydralazine affords strong, dose-dependent protection against the increases in plasma marker enzymes but not the hepatic glutathione depletion produced by allyl alcohol in mice. [5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 10 mM
DMSO : Insoluble


关键字: HIFs | Hydralazine Hydrochloride | HIF-PH | Hypoxia-inducible factors | antihypertensive | Hydralazine hydrochloride | Inhibitor | inhibit | orally active | HIF/HIF Prolyl-Hydroxylase | arterial vessel | Hydralazine

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相关库: Drug Repurposing Compound Library | Approved Drug Library | Transcription Factor-Targeted Compound Library | Drug-Fragment Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途