Stavudine (d4T) 是一种口服活性核苷逆转录酶抑制剂 ((NRTI))。Stavudine 具有抗HIV-1和HIV-2的活性。Stavudine 还抑制线粒体 DNA (mtDNA) 的复制。Stavudine 降低 NLRP3 炎症小体激活,调节淀粉样 β 自噬。Stavudine 诱导细胞凋亡。
生物活性 | Stavudine (d4T) is an orally activenucleosidereverse transcriptaseinhibitor(NRTI). Stavudine has activity againstHIV-1andHIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reducesNLRP3inflammasome activation and modulatesAmyloid-βautophagy. Stavudine inducesapoptosis[1][2][3][4]. |
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体外研究 (In Vitro) | Stavudine (d4T) (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[3]. Stavudine (d4T) (50 μM) inhibits the assembly of the NLRP3 inflammasome complex and down-regulates the phagocytosis of Aβ 42 by macrophages[3]. Stavudine (d4T) (10 μM, 7 or 14 days) significantly induced CEM cells apoptosis, especially after 14 days, and increases hydrogen peroxide levels[4].
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体内研究 (In Vivo) | Stavudine (d4T) (500 mg/kg, daily liquid, 2 weeks) can rapidly induce fat depletion and mild liver damage at high dose in male RjOrl Swiss mice[5].
Animal Model: | Male RjOrl Swiss mice weighing 0.028-0.03 kg[1] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(557.51 mM;Need ultrasonic) H2O : 16.67 mg/mL(74.35 mM;Need ultrasonic) 配制储备液 1 mM | 4.4601 mL | 22.3005 mL | 44.6010 mL | 5 mM | 0.8920 mL | 4.4601 mL | 8.9202 mL | 10 mM | 0.4460 mL | 2.2301 mL | 4.4601 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 120 mg/mL (535.21 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (11.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (11.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.15 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (11.15 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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