产品说明书
Ebselen
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同义名 : | SPI-1005;PZ-51;DR 3305;CCG-39161 |
| CAS号 : | 60940-34-3 | |
| 货号 : | A121080 | |
| 分子式 : | C13H9NOSe | |
| 纯度 : | 98% | |
| 分子量 : | 274.177 | |
| MDL号 : | MFCD00210937 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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]. | ||
| 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 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.65mL 0.73mL 0.36mL |
18.24mL 3.65mL 1.82mL |
36.47mL 7.29mL 3.65mL |
| 参考文献 |
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