(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮

生物活性靶点体外研究体内研究 (1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮试剂级价格

CAS号:39777-61-2
英文名:(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1,4-dien-3-one
中文名:(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮
CBNumber:CB82631480
分子式:C19H18O3
分子量:294.34
MOL File:39777-61-2.mol

(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮化学性质

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 :2-8°C
溶解度 :DMSO: 125 mg/mL (424.68 mM)
形态 :A solid
颜色 :Light yellow to yellow

(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮性质、用途与生产工艺

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
Target Value
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.