TFEB activator 1|39777-61-2|-陌孚医药/Medlife

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TFEB activator 1

目录号: PL09453 纯度: ≥99%

CAS No. :39777-61-2

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中文名称	TFEB activator 1
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-双(2-甲氧基苯基)-1,4-戊二烯-3-酮
英文名称	TFEB activator 1
英文别名	(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;TFEB activator 1
Cas No.	39777-61-2
分子式	C₁₉H₁₈O₃
分子量	294.34
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TFEB activator 1 是一种口服有效的，不依赖 mTOR 的 TFEB 激活剂。TFEB activator 1 显着促进 Flag-TFEB 的核易位，EC₅₀ 为 2167 nM。TFEB activator 1 在不抑制 mTOR 通路的情况下增强自噬 (autophagy)。TFEB activator 1 有潜力用于神经退行性疾病的研究。
生物活性	TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC 50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
性状	Solid
IC50 & Target[1][2]	EC50: 2167 nM (Flag-TFEB nuclear translocation)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Song JX, et al. A novel curcumin analog binds to and activates TFEB in vitro and in vivo independent of MTOR inhibition. Autophagy. 2016 Aug 2;12(8):1372-89.

溶解度数据	In Vitro: DMSO : 125 mg/mL (424.68 mM; Need ultrasonic)配制储备液

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