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。
生物活性 | IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally activeAMPKactivator that increasesAMPKphosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model[1][2]. IM156 is a potentoxidative phosphorylation (OXPHOS)inhibitor which can be used for the research of solid tumors[3]. |
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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].
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. |
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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].
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. |
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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 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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本网站选购。
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