T-448
目录号: PL09176 纯度: ≥98%
CAS No. :1597426-53-3
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中文名称
T-448
英文名称
T-448
英文别名
(E)-But-2-enedioic acid;3-[(1R,2S)-2-(cyclobutylamino)cyclopropyl]-N-(5-methyl-1,3,4-thiadiazol-2-yl;T-448
Cas No.
1597426-53-3
分子式
C21H24N4O5S
分子量
444.50
包装储存
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
T-448 是赖氨酸特异性去甲基化酶1 (LSD1,一种H3K4去甲基化酶) 不可逆的、口服有效的抑制剂,IC50 值为 22 nM。T-448能够加强原代培养的大鼠神经元中H3K4的甲基化。
生物活性
T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC 50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
性状
Solid
IC50 & Target[1][2]
IC50: 22 nM (LSD1).
体外研究(In Vitro)
T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction. has not independently confirmed the accuracy of these methods. They are for reference only.RT-PCR.
体内研究(In Vivo)
T-448 has minimal impact on the LSD1-GFI1B complex and a superior hematological safety profile in mice via the generation of a compact formyl-FAD adduct. T-448 increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction.
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg.
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
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[1]. Matsuda S, et al. T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice. Neuropsychopharmacology. 2018 Dec 22.
溶解度数据
In Vitro: DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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