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TFEB activator 1

CAS No. : 39777-61-2

MCE 国际站：TFEB activator 1

产品活性：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。

研究领域：Autophagy

作用靶点：Autophagy

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.

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.

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