IM156(Synonyms: HL156A; HL271 acetate)

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IM156 (Synonyms: HL156A; HL271 acetate) 纯度: 99.80%

IM156 (HL156A; HL271 acetate) 是二甲双胍 (HY-B0627) 的化学衍生物,是一种强效的,具有口服活性的 AMPK 激活剂。IM156 在动物模型中可缓解与年龄相关的认知障碍。IM156 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。

IM156(Synonyms: HL156A; HL271 acetate)

IM156 Chemical Structure

CAS No. : 1422365-94-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
50 mg ¥13500 In-stock
100 mg ¥19500 In-stock
200 mg   询价  
500 mg   询价  

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IM156 相关产品

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生物活性

IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model[1][2]. IM156 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)

IM156 (0.31-10 μM) phosphorylates AMPKα1 Thr172 in a dose- and time-dependent manner in NIH3T3 mouse fibroblast cells[1].
IM156 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)

IM156 does not affect metabolic regulation assessed by body weight, blood glucose, insulin levels and lipid metabolite content in mice with diet-induced obesity[1].
IM156 (50 mg/kg; for 2 months) does not affect body weight, general locomotion, or anxiety[2].
IM156 significantly attenuates the aging-induced decline in novel object recognition memory and spatial working memory[2].
IM156 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 (drinking water), for 2 months
Result: Attenuated age-related cognitive decline.

Clinical Trial

分子量

375.35

Formula

C15H20F3N5O3

CAS 号

1422365-94-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (266.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6642 mL 13.3209 mL 26.6418 mL
5 mM 0.5328 mL 2.6642 mL 5.3284 mL
10 mM 0.2664 mL 1.3321 mL 2.6642 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.66 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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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