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TML-6

CAS No. : 1462868-88-7

MCE 站：TML-6

产品活性：TML-6 是一种口服有效的姜黄素衍生物，抑制 β-淀粉样前体蛋白和 β-淀粉样蛋白 (Aβ) 的合成。TML-6 上调 Apo E，抑制 NF-κB 和 mTOR，并增加抗氧化 Nrf2 基因的活性。TML-6 具有用于阿尔茨海默氏病 (AD) 研究的潜力。

研究领域：Neuronal Signaling  |  NF-κB  |  PI3K/Akt/mTOR

作用靶点：Amyloid-β  |  NF-κB  |  mTOR  |  Keap1-Nrf2

In Vitro: TML-6 (0.65-5.24 ?g/mL; for 24 h) reduces the protein expression levels of APP and phospho-NF-κB, and induces the protein expression level of ApoE. TML-6 inhibits the mTOR signaling pathway through the suppression of phospho-mTOR.
TML-6 (0.31, 0.63, 2.5, 5, 10, 20 μM; 24 h) reveals no cytotoxicity in Huh-7 cells at concentrations below 5 μM and has an IC₅₀ of 4.19 ?g/mL (8 μM).
TML-6 (1.05, 2.09, 3.14, 4.19 μg/mL; 24 h) reduces the production of Aβ40 and Aβ42 between 1.05, 2.09 and 3.14 μg/mL (equal to 2, 4 and 6 μM) in a dose-dependent manner in N2a/APPswe cell.
TML-6 can exhibit transcriptional activation of the Nrf2 gene in a dose-dependent manner, with the highest activity at a concentration of 1.32 ?g/mL.

In Vivo: TML-6 (diet; 150 mg/kg/day; for four months) treatment results in significant improvement in learning, suppression of the microglial activation marker Iba-1, and reduction in Aβ in the brain.
TML-6 (oral; 150 mg/kg) has a T_1/2 of 1.27 hours, a C_max of 35.9 ng/mL and an AUC of 177 ng?hr/mL.

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