化合物 MK-28
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- CAS号:
- 864388-65-8
- 英文名:
- Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone
- 英文别名:
- MK-28;Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone;4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol;4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol , MK-28
- 中文名:
- 化合物 MK-28
- 中文别名:
- 化合物 MK-28;4-((2-(4,6-二苯基嘧啶-2-基)-2-甲基亚肼基)甲基)苯-1,2-二酚
- CBNumber:
- CB88131612
- 分子式:
- C24H20N4O2
- 分子量:
- 396.44
- MOL File:
- 864388-65-8.mol
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化合物 MK-28化学性质
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沸点:
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658.4±65.0 °C(Predicted)
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密度:
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1.22±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 12.5 mg/mL (31.53 mM)
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酸度系数(pKa):
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8.35±0.35(Predicted)
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形态:
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Solid
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颜色:
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Light yellow to yellow
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水溶解性:
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Water: < 0.1 mg/mL (insoluble)
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化合物 MK-28性质、用途与生产工艺
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。
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.
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Cell Line:
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ST
Hdh
Q
111/111
cells.
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Concentration:
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0-100 μM.
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Incubation Time:
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48 h.
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Result:
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Rescued cells from ER stress-induced apoptosis.
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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.
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Animal Model:
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R6/2 mice.
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Dosage:
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1 mg/kg.
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Administration:
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IP, daily for 28 days.
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Result:
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Incerased the survival.
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化合物 MK-28
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/08/19 | HY-137207 | MK-28 | | 1 mg | 1364元 |
| 2024/08/19 | HY-137207 | MK-28 | 864388-65-8 | 5mg | 3000元 |
864388-65-8, 化合物 MK-28 相关搜索:
- 4-((2-(4,6-二苯基嘧啶-2-基)-2-甲基亚肼基)甲基)苯-1,2-二酚
- 化合物 MK-28
- 864388-65-8
- 4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol
- 4-((2-(4,6-Diphenylpyrimidin-2-yl)-2-methylhydrazineylidene)methyl)benzene-1,2-diol , MK-28
- MK-28
- Benzaldehyde, 3,4-dihydroxy-, 2-(4,6-diphenyl-2-pyrimidinyl)-2-methylhydrazone