| 产品描述: | Lixumistat (HL271) hydrochloride (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin , is a potent AMPK activator that increases AMPK phosphorylation. Lixumistat hydrochloride attenuates aging-associated cognitive impairment in animal model. Lixumistat hydrochloride is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors. |
| 靶点: |
AMPK, OXPHOS |
| 体外研究: |
Lixumistat (hydrochloride) does not affect metabolic regulation assessed by body weight, blood glucose, insulin levels and lipid metabolite content in mice with diet-induced obesity[1]. Lixumistat (hydrochloride) (50 mg/kg; for 2 months) does not affect body weight, general locomotion, or anxiety[2]. Lixumistat (hydrochloride) significantly attenuates the aging-induced decline in novel object recognition memory and spatial working memory[2]. Lixumistat (hydrochloride) significantly increases AMPK activation in the hippocampus of aged mice[2]. |
| 体内研究: |
Lixumistat hydrochloride (0.31-10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells. Lixumistat hydrochloride does not affect the expression of key factors involved in glucose homeostasis such as glucose-6-phosphatase (G6pase) or phosphoenolpyruvate carboxykinase 1 (Pck1). |
| 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. |
| 保存条件: |
-80°C 6个月; -20°C 1个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.843 ml |
14.214 ml |
28.428 ml |
| 5 mM |
0.569 ml |
2.843 ml |
5.686 ml |
| 10 mM |
0.284 ml |
1.421 ml |
2.843 ml |
| 50 mM |
0.057 ml |
0.284 ml |
0.569 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |