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Lixumistat acetate

MCE China：Lixumistat acetate

Brand：MedChemExpress (MCE)

Cat. No.HY-136093A

CAS：1422365-94-3

Synonyms：IM156; HL156A; HL271 acetate

Purity：99.88%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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. Lixumistat (acetate) is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.

In Vitro：Lixumistat (acetate) (0.31-10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells[1]. Lixumistat (acetate) does not affect the expression of key factors involved in glucose homeostasis such as glucose-6-phosphatase (G6pase) or phosphoenolpyruvate carboxykinase 1 (Pck1)[1].

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].

IC50 & Target：AMPK[1][2], OXPHOS[3] In Vitro Lixumistat (acetate) (0.31-10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells[1]. Lixumistat (acetate) does not affect the expression of key factors involved in glucose homeostasis such as glucose-6-phosphatase (G6pase) or phosphoenolpyruvate carboxykinase 1 (Pck1)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Lixumistat acetate Related Antibodies Western Blot Analysis[1] Cell Line: NIH3T3 cells

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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.  [Content Brief]

[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.  [Content Brief]

[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.