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。
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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。 |
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]. |
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 |
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 |