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编 号:F128829
分子式:C10H11N2NaO4
分子量:246.2
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生物活性:
Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against HIV-1 and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.

体内研究:
Stavudine (d4T) sodium (500 mg/kg, daily liquid, 2 weeks) can rapidly induce fat depletion and mild liver damage at high dose in male RjOrl Swiss mice.Animal Model:Male RjOrl Swiss mice weighing 0.028-0.03 kg
Dosage:500 mg/kg
Administration:Daily liquid; 2 weeks
Result:Reduced fat weight gain by 58%, 5.7 g in the control group and 4.9 g in the d4T treated group.Significantly elevated plasma ALT and LDH levels.Reduced plasma acetoacetic acid and beta-hydroxybutyric acid levels.Reduced liver and muscle mtDNA levels at high dose concentration of 500 mg/kg.

体外研究:
Stavudine (d4T) sodium (50 μM) significantly reduces the expression of the NLRP3 inflammasome gene, IL-18 production and Aβ 42-stimulated cellular production of IL-1β in THP-1 derived macrophages.Stavudine (d4T) sodium (50 μM) inhibits the assembly of the NLRP3 inflammasome complex and down-regulates the phagocytosis of Aβ 42 by macrophages.Stavudine (d4T) sodium (10 μM, 7 or 14 days) significantly induced CEM cells apoptosis, especially after 14 days, and increases hydrogen peroxide levels.
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