MK-28|cas:864388-65-8|西域试剂

MK-28,99.50%

产品编号：Bellancom-137207| CAS NO：864388-65-8| 分子式：C₂₄H₂₀N₄O₂| 分子量：396.44

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-137207	￥3000.00	杭州北京（现货）
Bellancom-137207	￥4800.00	杭州北京（现货）
Bellancom-137207	￥14000.00	杭州北京（现货）
Bellancom-137207	￥21000.00	杭州北京（现货）

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MK-28

产品介绍

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 selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.

体外研究

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.
ATF4 protein levels are increased signifcantly, up to 2.5-fold, in STHdhQ^111/111 cells 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.
MK-28 has little or no efect on EIF2AK1 (HRI) or EIF2AK2 (PKR), but it activats EIF2AK4 (GCN2).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis.

Cell Line:	STHdhQ^111/111 cells.
Concentration:	0-100 μM.
Incubation Time:	48 h.
Result:	Rescued cells from ER stress-induced apoptosis.

体内研究
(In Vivo)

MK-28 (10 mg/kg, IP, single dose) shows a maximum concentration (C_max) of 105ng/ml and 30min half-life in plasma, 40 min afer the IP injection.
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.
MK-28 (Transient subcutaneous delivery) significantly improves motor and executive functions and delayed death onset in R6/2 mice, showing no toxicity.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	R6/2 mice.
Dosage:	1 mg/kg.
Administration:	IP, daily for 28 days.
Result:	Incerased the survival.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	R6/2 mice.
Dosage:	1 mg/kg.
Administration:	IP, daily for 28 days.
Result:	Incerased the survival.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	R6/2 mice.
Dosage:	1 mg/kg.
Administration:	IP, daily for 28 days.
Result:	Incerased the survival.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (31.53 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液