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Lixumistat acetate {[allProObj[0].p_purity_real_show]}

货号:A1365556 同义名: IM156;HL156A

Lixumistat acetate是二甲双胍的衍生物,是一种强效的,具有口服活性的 AMPK 激活剂。可以缓解与年龄相关的认知障碍,并作为一种有效的氧化磷酸化(OXPHOS)抑制剂,适用于实体肿瘤研究。

Lixumistat acetate 化学结构 CAS号:1422365-94-3
Lixumistat acetate 化学结构
CAS号:1422365-94-3
Lixumistat acetate 3D分子结构
CAS号:1422365-94-3
Lixumistat acetate 化学结构 CAS号:1422365-94-3
Lixumistat acetate 3D分子结构 CAS号:1422365-94-3
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Lixumistat acetate 纯度/质量文件 产品仅供科研

货号:A1365556 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 AMPK 其他靶点 纯度
WZ4003 ++++

NUAK1, IC50: 20 nM

NUAK2, IC50: 100 nM

98+%
Dorsomorphin ++

AMPK, Ki: 109 nM

99%
HTH-01-015 +++

NUAK1 , IC50: 100 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Lixumistat acetate 生物活性

描述 Lixumistat acetate, a chemical derivative of Metformin, is a potent and orally active activator of AMP-activated protein kinase (AMPK), leading to increased AMPK phosphorylation. Lixumistat (acetate) mitigates aging-related cognitive impairment in animal models [1][2]. Lixumistat (acetate) is a potent inhibitor of oxidative phosphorylation (OXPHOS) suitable for solid tumor research [3].
体内研究

Lixumistat (acetate) has no impact on metabolic regulation as assessed by body weight, blood glucose, insulin levels, and lipid metabolite content in mice with diet-induced obesity [1].

Lixumistat (acetate) (50 mg/kg; for 2 months) does not alter body weight, general locomotion, or anxiety levels [2].

Lixumistat (acetate) effectively reduces the aging-induced decline in both novel object recognition memory and spatial working memory [2].

Lixumistat (acetate) markedly enhances AMPK activation in the hippocampus of aged mice [2].

体外研究

Lixumistat (acetate) (0.31-10 μM) induces phosphorylation of AMPKα1 at Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells [1].

Lixumistat (acetate) does not alter the expression of crucial glucose homeostasis enzymes, including glucose-6-phosphatase (G6pase) and phosphoenolpyruvate carboxykinase 1 (Pck1) [1].

Lixumistat acetate 参考文献

[1]Row H, et al. HL271, a novel chemical compound derived from metformin, differs from metformin in its effects on the circadian clock and metabolism. Biochem Biophys Res Commun. 2016 Jan 15;469(3):783-9.

[2]Bang E, et al. The Improving Effect of HL271, a Chemical Derivative of Metformin, a Popular Drug for Type II Diabetes Mellitus, on Aging-induced Cognitive Decline. Exp Neurobiol. 2018 Feb;27(1):45-56.

[3]Sun Young Rha, et al. Phase I study of IM156, a novel potent biguanide oxidative phosphorylation (OXPHOS) inhibitor, in patients with advanced solid tumors. Journal of Clinical Oncology 38(15_suppl):3590-3590.

Lixumistat acetate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.64mL

5.33mL

2.66mL

Lixumistat acetate 技术信息

CAS号1422365-94-3
分子式C15H20F3N5O3
分子量 375.346
别名 IM156;HL156A;HL271 acetate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 50 mg/mL(133.21 mM),配合低频超声,并水浴加热至45℃助溶,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

动物实验配方
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