HL271(Synonyms: IM156 hydrochloride; HL156A hydrochloride)

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HL271 (Synonyms: IM156 hydrochloride; HL156A hydrochloride)

HL271 (IM156 hydrochloride) 是二甲双胍 (HY-B0627) 的化学衍生物，是一种强效的 AMPK 激活剂，能增加 AMPK 的磷酸化水平。HL271 在动物模型中可缓解与年龄相关的认知障碍。HL271 是一种有效的氧化磷酸化 (OXPHOS) 抑制剂，可用于实体肿瘤的研究。

HL271(Synonyms: IM156 hydrochloride; HL156A hydrochloride)

HL271 Chemical Structure

CAS No. : 1422365-52-3

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HL271 的其他形式现货产品:

IM156

生物活性

HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model[1][2]. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors[3].

IC50 & Target

AMPK[1][2], OXPHOS[3]
体外研究
(In Vitro)

HL271 (0.31-10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells[1].
HL271 does not affect the expression of key factors involved in glucose homeostasis such as glucose-6-phosphatase (G6pase) or phosphoenolpyruvate carboxykinase 1 (Pck1)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: NIH3T3 cells
Concentration: 0.31 μM, 0.62 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 4 hours
Result: Significantly increased the AMPK phosphorylation rate.

体内研究
(In Vivo)

HL271 does not affect metabolic regulation assessed by body weight, blood glucose, insulin levels and lipid metabolite content in mice with diet-induced obesity[1].
HL271 (50 mg/kg; for 2 months) does not affect body weight, general locomotion, or anxiety[2].
HL271 significantly attenuates the aging-induced decline in novel object recognition memory and spatial working memory[2].
HL271 significantly increases AMPK activation in the hippocampus of aged mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice (young group/12-16 weeks, old groups/20-22 months)[2]
Dosage: 50 mg/kg
Administration: Oral administration (in drinking water), for 2 months
Result: Attenuated age-related cognitive decline.

Clinical Trial

分子量

351.76

Formula

C13H17ClF3N5O
CAS 号

1422365-52-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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