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39777-61-2

中文名称 (1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮
英文名称 (1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1,4-dien-3-one
CAS 39777-61-2
分子式 C19H18O3
分子量 294.34
MOL 文件 39777-61-2.mol
更新日期 2023/12/18 22:09:24
39777-61-2 结构式 39777-61-2 结构式

基本信息

中文别名
(1E,4E)-1,5-二(2-甲氧基)-1,4-二烯基-3-戊酮
(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮
英文别名
RPN77612
TFEB activator 1
Curcumin analog C1
Curcumin analog compound C1
Curcumin analog C1(TFEB activator 1 )
(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1
1,5-Bis-(2-methoxy-phenyl)-penta-1,4-dien-3-one
(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1,4-dien-3-one
(1E,4E)-1,5-Bis(2-methoxyphenyl)-1,4-pentadien-3-one
1,4-Pentadien-3-one, 1,5-bis(2-Methoxyphenyl)-, (1E,4E)-
所属类别
生物:抑制剂激活剂

物理化学性质

熔点120-122 °C(Solv: ethanol (64-17-5); water (7732-18-5))
沸点467.2±40.0 °C(Predicted)
密度1.128±0.06 g/cm3(Predicted)
储存条件Sealed in dry,2-8°C
溶解度DMSO: 125 mg/mL (424.68 mM)
形态固体

常见问题列表

生物活性
Curcumin analog C1 (Curcumin analog Compound C1)是有效的 transcription factor EB (TFEB) 激活剂,有望用于预防或治疗阿尔茨海默氏病。
靶点
TargetValue
TFEB
()
体外研究

TFEB activator 1 (Compound C1) activates TFEB (transcription factor EB) by directly binding to TFEB and promotes its entry into the nucleus, without affecting TFEB phosphorylation or inhibiting the activities of MTOR and MAPK1/ERK2-MAPK3/ERK1.
TFEB activator 1 (1 μM; for 12 h) significantly increases the levels of LC3B-II, the lipidated and phagophore- or autophagosome-associated form of MAP1LC3B/LC3B (microtubule-associated protein 1 light chain 3 β) in N2a cells.
TFEB activator 1 (0.2-1 μM) dose-dependently increases the levels of LC3-II and SQSTM1/p62 (sequestosome 1) in N2a cells.

Western Blot Analysis

Cell Line: N2a cells
Concentration: 0, 0.2, 0.4, 0.6, 0.8 and 1 μM
Incubation Time: 12 hours
Result: Treatment dose-dependently increased the levels of LC3-II and SQSTM1/p62 (sequestosome 1).
体内研究

The medium lethal dose (LD 50 ) value of TFEB activator 1 (Compound C1) is 175 mg/kg in the acute toxicity assay (single-dose i.v. tail vein injection; in rats) .
Short-term oral administration of TFEB activator 1 (low dosage 10 mg/kg and high dosage 25 mg/kg; for 24 h) dose-dependently increases the expression of LC3B-II and TFEB in the liver, frontal cortex and striatum of the brain.
Chronic administration of TFEB activator 1 (10 mg/kg per day; orally administered by gavage) activates TFEB and enhances autophagy in rat brains.

Animal Model: Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g
Dosage: 10 mg/kg and 25 mg/kg
Administration: Short-term oral administration; for 24 hours
Result: Activated TFEB and enhanced autophagy and lysosome biogenesis in rat brain.
Animal Model: Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g
Dosage: 10 mg/kg
Administration: Chronic oral administration; daily; for 21 days
Result: Activated TFEB and enhanced autophagy in rat brains.
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