化合物 MK-28
- CAS号:864388-65-8
- 英文名:Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone
- 中文名:化合物 MK-28
- CBNumber:CB88131612
- 分子式:C24H20N4O2
- 分子量:396.44
- MOL File:864388-65-8.mol
- 沸点 :658.4±65.0 °C(Predicted)
- 密度 :1.22±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 12.5 mg/mL (31.53 mM)
- 酸度系数(pKa) :8.35±0.35(Predicted)
- 形态 :Solid
- 颜色 :Light yellow to yellow
- 水溶解性 :Water: < 0.1 mg/mL (insoluble)
化合物 MK-28性质、用途与生产工艺
- 生物活性 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。
-
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 ST Hdh Q 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).
Apoptosis Analysis.
Cell Line: ST Hdh Q 111/111 cells. Concentration: 0-100 μM. Incubation Time: 48 h. Result: Rescued cells from ER stress-induced apoptosis. -
体内研究
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.
Animal Model: R6/2 mice.
Dosage: 1 mg/kg. Administration: IP, daily for 28 days. Result: Incerased the survival.
- 更新日期：2024/04/30
- 产品编号：HY-137207
- 产品名称：MK-28
- CAS编号：
- 包装：1 mg
- 价格：1364元
- 更新日期：2024/04/30
- 产品编号：HY-137207
- 产品名称：MK-28
- CAS编号：864388-65-8
- 包装：5mg
- 价格：3000元
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：52927
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
