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AICAR

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Catalog No.
A8184
AMPK 激活剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
50mg
¥ 400.00
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200mg
¥ 1,200.00
现货
1g
¥ 3,500.00
现货

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Background

AICAR is a cell-permeable, allosteric activator of AMP-activated protein kinase (AMPK).

AMPK is a heterodimeric protein serine/threonine kinase that regulates the energy status of cells to protect cell from metabolic stress. AMPK phosphorylates various metabolic enzymes to activate catabolic pathways (e.g. ketogenesis) and block anabolic pathways (e.g. protein synthesis).

In rat primary astrocytes, microglia, and peritoneal macrophages, AICAR does-dependently inhibits the LPS-induced production of TNFα, IL-1β, and IL-6. AICAR treatment also blocks LPS-induced nitrite production and iNOS gene expression in those cells in a dose-dependent manner by activation of AMPK. Moreover, AICAR inhibits the LPS-induced C/EBP nuclear relocation via downregulating the expression of C/EBP-δ. [1]

In LPS-injected rats, AICAR treatment abolishes LPS-mediated increased levels of IL-1β and IFN-γ in serum. AICAR treatment also strongly inhibits the LPS-induced expression of iNOS in peritoneal macrophages isolated from these rats. Furthermore, the intraperitoneal injection of LPS significantly induces the expression of TNFα, IL-1β, and IFN-γ message in the rat spleen.

Reference:
1.  Giri S, Nath N, Smith B 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.

文献引用

1. Wei Q, Zhang B, et al. "Maslinic Acid Inhibits Colon Tumorigenesis by the AMPK-mTOR Signaling Pathway." J Agric Food Chem. 2019 Apr 17;67(15):4259-4272. PMID:30913881
2. Chen X, Han Y, et al. "Disulfide-bond A oxidoreductase-like protein protects against ectopic fat deposition and lipid-related kidney damage in diabetic nephropathy." Kidney Int. 2019 Feb 12. pii: S0085-2538(18)30899-8. PMID:30791996
3. Xu N, Wang Q, et al. "Fenofibrate improves vascular endothelial function and contractility in diabetic mice." Redox Biol. 2018 Oct 1;20:87-97. PMID:30296701

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt258.23
Cas No.2627-69-2
FormulaC9H14N4O5
SynonymsGP 1-110
Solubility≥12.9 mg/mL in DMSO, ≥52.9 mg/mL in H2O, <1.2 mg/mL in EtOH
Chemical Name5-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]imidazole-4-carboxamide
SDFDownload SDF
Canonical SMILESCC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

大鼠原代星形胶质细胞、小胶质细胞和巨噬细胞

制备方法

在DMSO中的溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.01 ~ 1 mM;2小时

实验结果

在大鼠原代星形胶质细胞、小胶质细胞和巨噬细胞中,AICAR呈剂量依赖性地抑制LPS诱导的TNFα、IL-1β和IL-6合成。

动物实验 [1]:

动物模型

注射LPS的大鼠

给药剂量

100 mg/kg;腹腔注射

实验结果

在注射LPS的大鼠中,AICAR阻止LPS介导的血清IL-1β和IFN-γ水平上升。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Giri S, Nath N, Smith B 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.

质量控制

化学结构

AICAR

相关生物数据

AICAR

相关生物数据

AICAR

相关生物数据

AICAR