Semagacestat | LY450139 | γ-secretase Inhibitor | AmBeed-信号通路专用抑制剂

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Semagacestat {[allProObj[0].p_purity_real_show]}

货号：A892738 同义名： LY450139

Semagacestat is an inhibitor of γ-secretase. It inhibits Aβ42, Aβ38, Aβ40 and the Notch signaling with IC50 of 10 nM, 12 nM, 12.1 nM and 14.1 nM.

Semagacestat 化学结构
CAS号：425386-60-3

Semagacestat 3D分子结构
CAS号：425386-60-3

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Semagacestat 纯度/质量文件产品仅供科研

货号：A892738 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

Semagacestat 生物活性

描述

Semagacestat is a γ-secretase inhibitor with efficacy in multiple cellular and animal models, with IC50 values of 10.9nM, 12.1nM, 12nM, 14.1nM for secretion of Aβ42, Aβ40, Aβ38 and Notch, respectively, and EC50 value of 16nM forβ-CTF production. Exposure to Semagacestat at concentration ranging in 3.2, 16, 80, 2000, and 10,000 nM for 24 h led a concentration-dependent increase of β-CTF and α-CTF in H4 cells stably overexpressing human wild-type APP. It is regarded as a candidate drug for a causal therapy against Alzheimer's disease and showed blood-brain barrier permeability. Oral administration of semagacestat at dose of 1mg for 8 days significantly ameliorated spatial working memory deficits (shown by Y-maze) in Tg2576 mice (5.5-monthold) on day 1, but not on day 8. Both reduction of hippocampal Aβ42/Aβ40 by 22–23% and elevation of β-CTF by 162% could be observed in Tg2576 mice after dose of 10mg. A subcutaneous injection of semagacestat at dose of 5 mg/kg immediately after traumatic brain injury and once daily for 3 consecutive days post-traumatic brain injury attenuated neurotrauma and neurogenic acute lung injury in rats due to reducing the accumulation of hypertrophic microglia in the vicinity of the lesion.

Semagacestat 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
African green monkey CV1 cells		Function assay		Inhibition of gamma-secretase expressed in african green monkey CV1 cells coexpressing Gal4 DNA-binding/transactivation domain assessed as inhibition of notch processing by luciferase reporter assay, IC50=0.31623 μM	20056541
CHO cells		Function assay		Inhibition of gamma-secretase in CHO cells assessed expressing APPSw assessed as inhibition of amyloid beta(1 to x) secretion after overnight incubation by ELISA, ED50=0.015 μM	23713656
human SH-SY5Y cells		Function assay		Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells, IC50=0.038 μM	19694467

Semagacestat 动物研究

Dose	Mice: 3 mg/kg - 30 mg/kg^[1] (p.o.); 1000 mg/kg^[4] (s.c. BID or p.o.) Guinea pig: 0.2 mg/kg- 60 mg/kg^[5] (p.o.)
Administration	p.o., s.c.

Semagacestat 参考文献

[1]Mitani Y, Yarimizu J, et al. Differential effects between γ-secretase inhibitors and modulators on cognitive function in amyloid precursor protein-transgenic and nontransgenic mice. J Neurosci. 2012 Feb 8;32(6):2037-50.

[2]Lanz TA, Karmilowicz MJ, et al. Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139. J Pharmacol Exp Ther. 2006 Nov;319(2):924-33. Epub 2006 Aug 18.

[3]Lin HJ, Hsu CC, et al. Gamma-Secretase Inhibitors Attenuate Neurotrauma and Neurogenic Acute Lung Injury in Rats by Rescuing the Accumulation of Hypertrophic Microglia. Cell Physiol Biochem. 2017;44(5):1726-1740.

Semagacestat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.77mL

0.55mL

0.28mL

13.83mL

2.77mL

1.38mL

27.67mL

5.53mL

2.77mL

Semagacestat 技术信息

CAS号	425386-60-3
分子式	C₁₉H₂₇N₃O₄
分子量	361.435

别名	LY450139
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(290.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

方案一

方案二

动物实验配方

0.5% methylcellulose+water 30 mg/mL suspension

Semagacestat {[allProObj[0].p_purity_real_show]}

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Semagacestat 生物活性

Semagacestat 细胞研究

Semagacestat 动物研究

Semagacestat 参考文献

Semagacestat 实验方案

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Semagacestat {[allProObj[0].p_purity_real_show]}

Semagacestat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Semagacestat 质控信息

Semagacestat 生物活性

Semagacestat 细胞研究

Semagacestat 动物研究

Semagacestat 参考文献

Semagacestat 实验方案

Semagacestat 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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