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Lixumistat (IM156; HL156A; HL271) acetate, a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. Lixumistat (acetate) attenuates aging-associated cognitive impairment in animal model[1][2]. Lixumistat (acetate) is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors[3]. | [in vivo]
Lixumistat (acetate) 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 (acetate) (50 mg/kg; for 2 months) does not affect body weight, general locomotion, or anxiety[2].
Lixumistat (acetate) significantly attenuates the aging-induced decline in novel object recognition memory and spatial working memory[2].
Lixumistat (acetate) significantly increases AMPK activation in the hippocampus of aged mice[2].
| Animal Model: | C57BL/6J mice (young group/12-16 weeks, old groups/20-22 months)[2] | | Dosage: | 50 mg/kg | | Administration: | Oral administration (drinking water), for 2 months | | Result: | Attenuated age-related cognitive decline. |
| [References]
[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. DOI:10.1016/j.bbrc.2015.11.069
[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. DOI:10.5607/en.2018.27.1.45
[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. |
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