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AICAR (Synonyms: 阿卡地新; Acadesine; AICA Riboside)

目录号: PC15450 纯度: ≥98%

CAS No. :2627-69-2

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PC15450-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

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中文名称

AICAR

中文别名

阿卡地新;5-氨基-1-beta-D-呋喃核糖基-1H-咪唑-4-甲酰胺;5-氨基咪唑-4-甲酰胺-1-B-D-呋喃核糖苷;5-氨基咪唑-4-甲酰胺-1-β-D-呋喃核糖苷;5-氨基咪唑-4-甲酰胺核苷酸转甲酰酶;阿卡地辛;阿卡地新 Acadesine;阿卡地新(AICAR);5-氨基咪唑-4-甲酰胺盐酸盐;氨鲁米特

英文名称

AICAR

英文别名

5-Amino-1-beta-D-ribofuranosyl-1H-imidazole-4-carboxamide;Aicar;Acadesine;5-Aminoimidazole-4-carboxamide-1-β-D-ribofuranoside;AICAR(Acadesine,NSC 105823,AICA-Riboside,ATH001,GP 1-110,Z-Riboside ,Acadra®);AIC-Riboside;5-amino-4-imidazole carboxamide ribonucleoside;5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside;Acadesine,AICA;AICA Riboside;AICA-RIBOSIDE;AMPK;Arasine;GP 1-110;Z-RIBOSIDE;5-Aminoimidazole-4-carboxamide 1-β-D-ribofuranoside;N1-(β-D-Ribofuranosyl)-5-aminoimidazole-4-carboxamide;Acadesina;Acadesinum;AICAR (Acadesine);Protara;5-Amino-1-beta-D-ribofuranosylimidazole-4-carboxamide;5-Aminoimidazole-4-carboxamide-1-beta-riboside;5-Amino-1-beta-D-ribofuranosyl-4-imidazolecarboxamide;5-Amino-4-imidazolecarboxamide ribofuranoside;5-Aminoimidazole-4-carboxamide ribonucleoside;C9H14N4O5;NSC105823;5-Amino

Cas No.

2627-69-2

分子式

C₉H₁₄N₄O₅

分子量

258.23

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.

性状

Solid

IC50 & Target[1][2]

AMPK

Human Endogenous Metabolite

Autophagy

Mitophagy

体外研究(In Vitro)

HepG2 cells are treated with various concentrations of AICAR (0.1-1.0 mM) for 12, 24, and 48 h, respectively. The expression level of IR-β significantly decreases with 0.25, 0.5, and 1.0 mM of AICAR at 48 h to 50%, 53%, and 46% of the control, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Fourteen-week-old male, lean (L; 31.3 g body wt) wild-type andob/ob (O; 59.6 g body wt) mice are injected with the AMP-activated kinase (AMPK) activator AICAR (A) at 0.5 mg/g per day or saline control (C) for 14 days. At 24 h after the last injection (including a 12-h fast), all mice are killed, and the plantar flexor complex muscle (gastrocnemius, soleus, and plantaris) is excised for analysis. Muscle mass is lower in OC (159±12 mg) than LC, LA, and OA (176±10, 178±9, and 166±16 mg, respectively) mice, independent of a body weight change. The kidney weight is significantly higher in the untreated group when compared with both the exercise and AICAR (0.5 mg/g body wt) groups. The heart weight is higher in the exercise group than in the other groups, whereas the liver weight is significantly higher in the AICAR-treated group when compared with the exercise and untreated groups.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Nakamaru K, et al. AICAR, an activator of AMP-activated protein kinase, down-regulates the IR expression in HepG2 cells. Biochem Biophys Res Commun. 2005 Mar 11;328(2):449-54 [Information]

[2]. Giri S, et al. 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside inhibits proinflammatory response in glial cells: a possible role of AMP-activated protein kinase. J Neurosci. 2004 Jan 14;24(2):479-87. [Information]

[3]. Drake JC, et al. AICAR treatment for 14 days normalizes obesity-induced dysregulation of TORC1 signaling and translational capacity in fasted skeletal muscle. Am J Physiol Regul Integr Comp Physiol. 2010 Dec;299(6):R1546-54. [Information]

[4]. Pold R, et al. Long-term AICAR administration and exercise prevents diabetes in ZDF rats.Diabetes. 2005 Apr;54(4):928-34. [Information]

[5]. Ajaybabu V Pobbati, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635. [Information]

溶解度数据

体外研究:

H₂O : 65 mg/mL (251.71 mM; Need ultrasonic and warming)

DMSO : ≥ 50 mg/mL (193.63 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8725 mL	19.3626 mL	38.7252 mL
5 mM	0.7745 mL	3.8725 mL	7.7450 mL
10 mM	0.3873 mL	1.9363 mL	3.8725 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 110 mg/mL (425.98 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (8.05 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.05 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.05 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (8.05 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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