Stavudine, a nucleoside analog, inhibits reverse transcriptase of HIV.
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描述 | Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI) known for its effectiveness against HIV-1 and HIV-2. Besides its antiviral properties, stavudine also inhibits mitochondrial DNA (mtDNA) replication, modulates autophagy related to Amyloid-β, reduces activation of the NLRP3 inflammasome, and induces apoptosis[1].[2].[3].[4]. |
体内研究 | Moreover, a high dose of stavudine (500 mg/kg, administered daily in liquid form for two weeks) has been shown to cause rapid fat depletion and mild liver damage in male RjOrl Swiss mice[5]. |
体外研究 | In laboratory experiments with THP-1 derived macrophages, stavudine at a concentration of 50 μM significantly lowers the expression of the NLRP3 inflammasome gene, reduces IL-18 production, and decreases IL-1β production stimulated by Aβ 42[3]. Additionally, at the same concentration, stavudine impedes the assembly of the NLRP3 inflammasome complex and reduces macrophage phagocytosis of Aβ 42[3]. When administered to CEM cells at 10 μM for either 7 or 14 days, stavudine notably induces apoptosis, particularly after 14 days, and raises hydrogen peroxide levels[4]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01192035 | HIV-1 | Phase 4 | Completed | - | Guinea-Bissau ... 展开 >> Centro de Tratamento Ambulatoria do Hospital Nacional Simão Mendes Bissau, Guinea-Bissau 收起 << |
NCT00119379 | HIV Infections ... 展开 >> Lipodystrophy Metabolic Diseases Nutrition Disorders 收起 << | Phase 2 | Completed | - | United States, Ohio ... 展开 >> University Hospitals of Cleveland Cleveland, Ohio, United States, 44106 收起 << |
NCT00005018 | HIV Infections | Phase 4 | Completed | - | United States, California ... 展开 >> East Bay AIDS Ctr Berkeley, California, United States, 94705 Pacific Oaks Research Beverly Hills, California, United States, 90211 Altamed Medical Health Services Los Angeles, California, United States, 90022 St Lukes Medical Group San Diego, California, United States, 92101 Pacific Horizons Med Group San Francisco, California, United States, 94115 United States, Florida Gary Richmond MD Fort Lauderdale, Florida, United States, 33316 Univ of Miami School of Medicine Miami, Florida, United States, 331361013 Saint Josephs Comprehensive Research Institute Tampa, Florida, United States, 33607 United States, Illinois Northstar Med Clinic Chicago, Illinois, United States, 60657 United States, Kentucky Univ of Kentucky Med Ctr Lexington, Kentucky, United States, 40536 United States, Massachusetts Boston Med Ctr / Evans - 556 Boston, Massachusetts, United States, 021182393 CRI of New England Brookline, Massachusetts, United States, 02445 United States, Nebraska Univ of Nebraska Medical Ctr Omaha, Nebraska, United States, 681985400 United States, New York Beth Israel Med Ctr New York, New York, United States, 10003 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10019 United States, North Carolina Univ of North Carolina / Infectious Disease Division Chapel Hill, North Carolina, United States, 27599 Univ of NC Infectious Diseases Wilmington, North Carolina, United States, 28402 United States, Pennsylvania Anderson Clinical Research Inc Reading, Pennsylvania, United States, 19604 United States, Rhode Island Miriam Hosp Providence, Rhode Island, United States, 02906 United States, South Carolina Burnside Clinic Columbia, South Carolina, United States, 29206 United States, Texas Univ of Texas Med Branch Galveston, Texas, United States, 77555 Univ of Texas / Thomas Street Clinic Houston, Texas, United States, 77030 United States, Virginia Hampton Roads Med Specialists Hampton, Virginia, United States, 23666 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.46mL 0.89mL 0.45mL |
22.30mL 4.46mL 2.23mL |
44.60mL 8.92mL 4.46mL |
CAS号 | 3056-17-5 |
分子式 | C10H12N2O4 |
分子量 | 224.213 |
别名 | d4T;BMY 27857;Zerit;Stavudinum;NSC 163661 |
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: 120 mg/mL(535.2 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 H2O: 15 mg/mL(66.9 mM),配合低频超声助溶 |
动物实验配方 |