TFEB activator 1|cas:39777-61-2|西域试剂

TFEB activator 1,99.72%

产品编号：Bellancom-135825| CAS NO：39777-61-2| 分子式：C₁₉H₁₈O₃| 分子量：294.34

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货号	价格	库存与货期
Bellancom-135825	￥650.00	杭州北京（现货）
Bellancom-135825	￥1000.00	杭州北京（现货）
Bellancom-135825	￥2000.00	杭州北京（现货）
Bellancom-135825	￥3500.00	杭州北京（现货）
Bellancom-135825	￥5500.00	杭州北京（现货）

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TFEB activator 1

产品介绍

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 EC₅₀ of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

The medium lethal dose (LD₅₀) 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (424.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3974 mL	16.9872 mL	33.9743 mL
5 mM	0.6795 mL	3.3974 mL	6.7949 mL
10 mM	0.3397 mL	1.6987 mL	3.3974 mL

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (21.23 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (21.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。