PKR-IN-C16 (Compound C16) 是一种特异的双链 RNA 依赖蛋白激酶 (PKR) 抑制剂。PKR-IN-C16 具有良好的神经保护作用，可挽救急性脑损伤。
| 生物活性 | PKR-IN-C16 (Compound C16) is a specificdouble-stranded RNA-dependent protein kinase(PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions[1]. |
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体外研究
(In Vitro) | PKR-IN-C16 (Compound C16) is able to unlock the translation blockade induced by PKR in primary neuronal cultures[1].
PKR-IN-C16 (0.1 or 0.3 μM; 24 h) shows protective effect against the neuronal cell death induced by endoplasmic reticulum stress in SH-SY5Y cells[1].
PKR-IN-C16 (1-1000 nM; 4 h) prevents not only PKR-phosphorylation but also the activation of caspase-3 induced by Amyloid β in SH-SY5Y cells[2].
Western Blot Analysis[2] | Cell Line: | Human SH-SY5Y cells | | Concentration: | 1, 10, 20, 200, 1000 nM | | Incubation Time: | 4 h | | Result: | Markedly reduces the level of phosphorylated PKR in the cells exposed to 20 μM Amyloid β. |
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体内研究
(In Vivo) | PKR-IN-C16 (Compound C16) (60 or 600 μg/kg; i.p.; 3 times) prevents not only the PKR-induced neuronal loss but also the inflammatory response in theQuinolinic acid(QA) (HY-100807) induced acute excitotoxic rat model[1]
| Animal Model: | Normotensive male Wistar rats, excitotoxic neuroinflammatory model, inflammation was induced by unilateral striatal injection of quinolinic acid (QA)[1] | | Dosage: | 60 or 600 μg/kg | | Administration: | Intraperitoneal injection; 24 h, 2 h before QA injection and 24 h post-QA injection | | Result: | Reduced expression of the active catalytic domain of the PKR, prevented increase
of IL-1β levels on the contralateral side (97% inhibition) at 600 μg/kg. Decreased by 47% the neuronal loss and by 37% the number of positive cleaved caspase-3 neurons induced by QA injection at 600 μg/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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 7.35 mg/mL(27.40 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 3.7273 mL | 18.6365 mL | 37.2731 mL | | 5 mM | 0.7455 mL | 3.7273 mL | 7.4546 mL | | 10 mM | 0.3727 mL | 1.8637 mL | 3.7273 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。 |
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