別名: 4-Phenylbutyric acid, NaPB 中文名稱:苯基丁酸鈉
4-PBA (Sodium Phenylbutyrate)是4-phenylbutyrate (4-PBA)或4-phenylbutyric acid的鹽形式。Sodium Phenylbutyrate是一種轉錄調節(jié)因子,通過調控HDAC活性來改變染色質結構從而發(fā)揮作用。
4-PBA (Sodium Phenylbutyrate) Chemical Structure
CAS: 1716-12-7
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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HT-29 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human HT-29 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 |
VA10 | Function assay | 4 mM | 24 hrs | Induction of CAMP mRNA expression in human VA10 cells at 4 mM after 24 hrs by RT-PCR analysis | 19770273 |
U937 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human U937 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 |
A498 | Function assay | 4 mM | 8 to 48 hrs | Induction of CAMP mRNA expression in human A498 cells at 4 mM after 8 to 48 hrs by RT-PCR analysis | 19770273 |
VA10 | Function assay | 4 mM | 24 hrs | Induction of DEFB1 mRNA expression in human VA10 cells at 4 mM after 24 hrs by RT-PCR analysis | 19770273 |
VA10 | Function assay | 4 mM | 24 hrs | Induction of LL-37 protein expression in human VA10 cells at 4 mM after 24 hrs by Western blotting | 19770273 |
VA10 | Function assay | 20 nM | 24 hrs | Induction of LL-37 protein expression in human VA10 cells at 20 nM after 24 hrs by Western blotting | 19770273 |
Hela | Function assay | Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay, Ki=6.34μM | 19520580 | ||
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產品描述 | 4-PBA (Sodium Phenylbutyrate)是4-phenylbutyrate (4-PBA)或4-phenylbutyric acid的鹽形式。Sodium Phenylbutyrate是一種轉錄調節(jié)因子,通過調控HDAC活性來改變染色質結構從而發(fā)揮作用。 | |
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靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Phenylbutyrate是一種公知的HDAC抑制劑,這增加了一些基因的基因轉錄,并且還發(fā)揮治療作用。Phenylbutyrate顯著衰減MPTP誘導的紋狀體多巴胺的損失和酪氨酸羥化酶陽性神經元的損失。[1] 在前列腺癌細胞中,Phenylbutyrate衰減凋亡拮抗劑的Bcl-X(L),雙鏈斷裂修復的蛋白質的DNA依賴性蛋白激酶,前列腺進展標記caveolin-1和促血管發(fā)生血管內皮生長因子的表達。在前列腺癌細胞中,Phenylbutyrate和電離輻射協(xié)同作用誘導細胞凋亡。 [2] |
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實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
Western blot | Survivin p38 / p-p38 / ERK / p-ERK / JNK / p-JNK |
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27274278 |
體內研究(In Vivo) | ||
體內研究活性 | 在轉基因G93AALS小鼠中,Phenylbutyrate顯著延長生存并改善臨床病理和表型。Phenylbutyrate可改善G93A小鼠中組蛋白去乙?;⒄T導核因子-κB(NF-κB的)p50,磷酸化的抑制亞基和β細胞淋巴瘤2(BCL-2)的表達,但降低了細胞色素c的和caspase表達。Phenylbutyrate表現磷酸化的IκB,易位的NF-κB的p50至細胞核,或直接乙酰化的NF-κB的p50。[3] 在亨廷頓氏?。℉D)的轉基因小鼠模型中,Phenylbutyrate增加腦組蛋白乙?;⒔档徒M蛋白甲基化水平,由免疫細胞化學和Western印跡評估。在紋狀體中,Phenylbutyrate增加泛素-蛋白酶體途徑的mRNA并下調凋亡性細胞死亡,活性胱天蛋白酶3的免疫反應性。[4] |
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NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
---|---|---|---|---|---|
NCT05983588 | Recruiting | Corticobasal Syndrome (CBS) |
Technical University of Munich |
December 12 2023 | Phase 2 |
NCT05019417 | Unknown status | Monocarboxylate Transporter 8 Deficiency |
Kaplan Medical Center|Weizmann Institute of Science |
June 30 2021 | Phase 2|Phase 3 |
NCT04937062 | Enrolling by invitation | STXBP1 Encephalopathy With Epilepsy SLC6A1 Neurodevelopmental Disorder|Developmental and Epileptic Encephalopathy |
Weill Medical College of Cornell University|Children''s Hospital Colorado|SLC6A1 Connect|STXBP1 Foundation|Clara Inspired|University of Pennsylvania Orphan Disease Center|Horizon Therapeutics |
March 1 2021 | Early Phase 1 |
NCT04421677 | Completed | Inclusion Body Myositis|Sporadic Inclusion Body Myositis |
University of Kansas Medical Center |
August 20 2020 | Phase 1 |
NCT02246218 | Completed | Urea Cycle Disorder |
Horizon Therapeutics LLC|Horizon Pharma Ireland Ltd. Dublin Ireland |
December 31 2014 | Phase 4 |
NCT01096095 | Withdrawn | Spinocerebellar Ataxia Type 3 |
Hospital de Clinicas de Porto Alegre|Funda??o de Amparo à Pesquisa do Estado do Rio Grande do Sul Brazil |
June 2010 | Phase 2 |
分子量 | 187.19 | 分子式 | C10H11O2.Na |
CAS號 | 1716-12-7 | SDF | Download 4-PBA (Sodium Phenylbutyrate) SDF |
Smiles | C1=CC=C(C=C1)CCCC(=O)[O-].[Na+] | ||
儲存條件(自收到貨起) | |||
體外溶解度 |
DMSO : 37 mg/mL ( (197.66 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : 37 mg/mL (197.66 mM) Ethanol : Insoluble |
摩爾濃度計算器 |
體內溶解度 現配現用,請按從左到右的順序依次添加,澄清后再加入下一溶劑 |
動物體內配方計算器 |
動物體內配方計算器(澄清溶液)
第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)
第二步:請輸入動物體內配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯系Selleck為您提供正確的澄清溶液配方)
計算結果:
工作液濃度: mg/ml;
DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,注:如該濃度超過該批次藥物DMSO溶解度,請先聯系Selleck);
體內配方配制方法:取μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。
體內配方配制方法:取μL DMSO母液,加入μL Corn oil,混勻澄清。
注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。
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