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/ Ebselen

依布硒 /Ebselen {[allProObj[0].p_purity_real_show]}

货号：A121080 同义名： SPI-1005;PZ-51

Ebselen is a small-molecule capsid inhibitor of HIV-1 replication with anti-inflammatory, anti-oxidant and cytoprotective activity.

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Ebselen 化学结构 CAS号：60940-34-3
Ebselen 化学结构
CAS号：60940-34-3
Ebselen 3D分子结构
CAS号：60940-34-3
Ebselen 化学结构 CAS号：60940-34-3
Ebselen 3D分子结构 CAS号：60940-34-3
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Ebselen 纯度/质量文件 产品仅供科研

货号：A121080 标准纯度： {[allProObj[0].p_purity_real_show]}
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Ebselen 生物活性

描述 The human immunodeficiency virus type 1 (HIV-1) capsid plays crucial roles in HIV-1 replication and thus represents an excellent drug target. Ebselen (SPI-1005) is a small-molecule capsid inhibitor of HIV-1 Replication with anti-inflammatory, anti-oxidant and cytoprotective activity. It also blocks infection of other retroviruses, such as Moloney murine leukemia virus and simian immunodeficiency virus, but displays no inhibitory activity against hepatitis C and influenza viruses[3]. Ebselen inhibited the infection of HIV isolate NL4.3 in HeLa-CD4-LTR-LacZ cells in a dose-dependent manner, with an EC50 of 1.99 ± 0.57 μM[3]. Ebselen is also a potent inhibitor of Insulin-degrading enzyme with IC50 of 14 nM[4]. In rat model of spinal cord injury (SCI), ebselen treatment (10 mg/kg, once daily for 3 days) increased the motor function of the hind limbs (BBB score), glutathione content, superoxide dismutase activity, catalase enzyme activity and decreased neuronal apoptosis ratio, compared with the SCI group[5].

Ebselen 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02779192 Noise Induced Hearing Loss Phase 2 Not yet recruiting October 2021 United States, Florida ... 展开 >> University of Miami Not yet recruiting Miami, Florida, United States, 33136 Contact: Michael Hoffer, MD          United States, Kansas University of Kansas Medical Center Not yet recruiting Kansas City, Kansas, United States, 66103 Contact: Hinrich Staecker, MD/PhD          United States, South Carolina MUSC Charleston, South Carolina, United States, 29425 United States, Texas University of Texas Southwestern Not yet recruiting Dallas, Texas, United States, 75390 Contact: Joe Kutz, MD          United States, Washington Sound Pharmaceuticals, Inc. Seattle, Washington, United States, 98103 收起 <<
NCT01451853 Lung Cancer H... 展开 >>ead and Neck Cancer Hearing Loss Ototoxicity Tinnitus Neuropathy 收起 << Phase 2 Not yet recruiting September 23, 2019 United States, Washington ... 展开 >> VA Puget Sound Health Care Not yet recruiting Seattle, Washington, United States, 98108 Contact: Tony S. Quang, M.D.    206-768-5356       Principal Investigator: Tony S Quang, M.D. 收起 <<
NCT03325790 Meniere's Disease Phase 2 Recruiting December 2018 United States, District of Col... 展开 >>umbia Georgetown University Recruiting Washington, District of Columbia, United States, 20057 Contact: Study Director          United States, Kentucky Advanced ENT & Allergy Recruiting Louisville, Kentucky, United States, 40207 Contact: Study Director          United States, New York ENT and Allergy Associates, LLP Recruiting New York, New York, United States, 10017 Contact: Study Director          United States, South Carolina MUSC Recruiting Charleston, South Carolina, United States, 29425 Contact: Study Director          United States, Texas UT Southwestern Recruiting Dallas, Texas, United States, 75390 Contact: Study Director          United States, Washington Northwest Ear, Inc. Recruiting Seattle, Washington, United States, 98104 Contact: Study Director 收起 <<

Ebselen 参考文献

[1]Thenin-Houssier S, de Vera IM, et al. Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2195-208.

[2]Pavon N, Correa F, et al. Ebselen induces mitochondrial permeability transition because of its interaction with adenine nucleotide translocase. Life Sci. 2015 Oct 15;139:108-13.

[3]Thenin-Houssier S, de Vera IM, Pedro-Rosa L, Brady A, Richard A, Konnick B, Opp S, Buffone C, Fuhrmann J, Kota S, Billack B, Pietka-Ottlik M, Tellinghuisen T, Choe H, Spicer T, Scampavia L, Diaz-Griffero F, Kojetin DJ, Valente ST. Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2195-208. doi: 10.1128/AAC.02574-15. PMID: 26810656; PMCID: PMC4808204.

[4]Leroux F, Bosc D, Beghyn T, Hermant P, Warenghem S, Landry V, Pottiez V, Guillaume V, Charton J, Herledan A, Urata S, Liang W, Sheng L, Tang WJ, Deprez B, Deprez-Poulain R. Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening. Eur J Med Chem. 2019 Oct 1;179:557-566. doi: 10.1016/j.ejmech.2019.06.057. Epub 2019 Jun 24. PMID: 31276900; PMCID: PMC6718346.

[5]Jia ZQ, Li SQ, Qiao WQ, Xu WZ, Xing JW, Liu JT, Song H, Gao ZY, Xing BW, He XJ. Ebselen protects mitochondrial function and oxidative stress while inhibiting the mitochondrial apoptosis pathway after acute spinal cord injury. Neurosci Lett. 2018 Jun 21;678:110-117. doi: 10.1016/j.neulet.2018.05.007. Epub 2018 May 4. PMID: 29733976.

Ebselen 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.65mL

0.73mL

0.36mL

18.24mL

3.65mL

1.82mL

36.47mL

7.29mL

3.65mL

Ebselen 技术信息

CAS号60940-34-3
分子式C13H9NOSe
分子量 274.177
别名 SPI-1005;PZ-51;DR 3305;CCG-39161
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(182.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Ebselen | SPI-1005;PZ-51;DR 3305;CCG-39161 | Iron death Inhibitor | Cyclooxygenase (COX) | Cyclooxygenase (COX) Inhibitor | NADH Peroxidase Inhibitor | Lipoxygenase Inhibitor | HIV | AmBeed-信号通路专用抑制剂 | Ebselen 纯度/质量文件 | Ebselen 生物活性 | Ebselen 临床数据 | Ebselen 参考文献 | Ebselen 实验方案 | Ebselen 技术信息

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