MK-28 是有效、选择性的PERK激动剂。MK-28 在小鼠中表现出良好的药代动力学特征，且能透过血脑屏障。
| 生物活性 | MK-28 is a potent and selectivePERKactivator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice[1]. |
体外研究
(In Vitro) | MK-28 (0-100 μM) shows PERK selectivity in vitro on a 391-kinase panel and rescues cells (but not PERK–/–cells) from ER stress-induced apoptosis[1].
ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ111/111cells at high MK-28 concentration. CHOP and GADD34 mRNA levels show a signifcant increase in both cell types, up to 10- and 5-fold respectively[1].
MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2)[1].
Apoptosis Analysis[1]. | Cell Line: | STHdhQ111/111cells. | | Concentration: | 0-100 μM. | | Incubation Time: | 48 h. | | Result: | Rescued cells from ER stress-induced apoptosis. |
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体内研究
(In Vivo) | MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (Cmax) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection[1].
MK-28 (1 mg/kg, IP, daily for 28 days) improves systemic function and survival in R6/2 mice and induces increased levels of eIF2α-P in the mouse brain striatum[1].
MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity[1].
| Animal Model: | R6/2 mice[1].
| | Dosage: | 1 mg/kg. | | Administration: | IP, daily for 28 days. | | Result: | Incerased the survival. |
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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 : 12.5 mg/mL(31.53 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL | | 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | | 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1.25 mg/mL (3.15 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (3.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 12.5 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。 *以上所有助溶剂都可在本网站选购。
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