AICAR (Acadesine), AMP 激活蛋白激酶、AMPK 激活剂

CAS: 2627-69-2 货号: A408470 分子式: C9H14N4O5 分子量: 258.23 EC号: 220-097-5
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级别和纯度: Moligand™ ? Moligand™ —— 阿拉丁的配体和生物活性小分子系列。适用于需要明确小分子工具的受体、通路和结合研究。 10mM in DMSO
别名
AICAR(阿卡地辛)
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
A408470-1ml
现货 Stock Image
¥199.90
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Moligand™ 级 ,适用于对基线干扰要求严格的色谱和分析工作流程。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。

概述

Acadesine导致ZMP的积累,Acadesine模仿AMP对AMPK和AMPK的刺激作用。An inhibitor of the transcription of PPARα, the coactivation of PPARα.

Information

AICAR (Acadesine) AICAR (Acadesine, NSC105823, AICA Riboside), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy . Phase 3.
In vitro

Acadesine (500 μM) increases the ZMP content in extracts of isolated hepatocytes after up to 30-40 min treatment, then remains fairly constant at approximately 4 nmol/g. Acadesine (500 μM) causes a transient 12-fold activation of AMPK at 15 min in rat hepatocytes and 2-3 fold activation of AMPK in adipocytes, without affecting levels of ATP, ADP or AMP. Acadesine (500 μM) causes a dramatic inhibition of both fatty acid and sterol synthesis in rat hepatocytes. Acadesine (500 μM) also causes a dramatic inactivation of HMG-CoA reductase. Acadesine induces apoptosis of B-CLL cells in a dose-dependent manner with EC50 of 380\u2009μM. Acadesine (0.5 mM) decreases cell viability of B-CLL cells from 20 representative patients from 68% to 26%. Acadesine (0.5 mM) induces caspase activation and cytochrome crelease from mitochondria. Uptake and phosphorylation of Acadesine (0.5 mM) are required to induce apoptosis and activate AMPK in B-CLL cells. Acadesine (2-4 mM) only slightly affects the viability of T cells from B-CLL patients, Acadesine (0.5 mM) remarkedly reduces viability of B cells but not T cells. [2] Acadesine triggers loss of cell metabolism in K562, LAMA-84 and JURL-MK1 and is also effective in killing imatinib-resistant K562 cells and Ba/F3 cells carrying the T315I-BCR-ABL mutation. The effect of Acadesine is abrogated by GF109203X and Ro-32-0432, both inhibitor of classical and new PKCs and accordingly, Acadesine triggers relocation and activation of several PKC isoforms in K562 cells. Acadesine dose-dependently inhibits K562 colony formation at day 10, the growth inhibitory effect of acadesine is already detected at 0.25 mM and is maximal at 2.5 mM. Acadesine causes a concentration-related reduction in CD18 expression on LPS-stimulated neutrophils in vitro. Acadesine significantly (1 mM) inhibits N-formyl-methionyl-leucyl-phenylalanine-induced granulocyte CD11b up-regulation by a mean of 61% in blood.

In vivo

Acadesine (50 mg/kg) significantly reduces tumor formation in a mouse xenograft model of K562 cells. Acadesine (10 mg/kg) results in higher fluid required to stabilize hemodynamics in pigs. Acadesine (10 mg/kg) inhibits LPS-induced protein permeability of pulmonary capillaries, peak inspiratory pressures on constant tidal volume and dead space ventilation in pigs.
Cell Data

cell lines:K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562

Concentrations:2.5 mM

Incubation Time:10 days

Powder Purity:≥99%

规格

别名
AICAR(阿卡地辛)
英文别名
NSC105823, AICA Riboside | 5-amino-1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-1H-imidazole-4-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AICAR (Acadesine)
生化机理
AICAR(Acadesine,NSC105823,AICA 核苷)是一种 AMPK 激活剂,可导致 ZMP 的积累,而 ZMP 可模拟 AMP 对 AMPK 和 AMPK 激酶的刺激作用。AICAR(Acadesine)可诱导有丝分裂。第 3 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激活剂
作用机制
AMP 激活蛋白激酶、AMPK 激活剂
名称和识别符
EC号
220-097-5
分子类型
小分子
Isomeric SMILES
C1=NC(=C(N1[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)N)C(=O)N
分子量
258.23
Reaxy-Rn
623893
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=623893&ln=

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高级数据

产品属性
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安全和危险性(GHS)
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危险声明

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。

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P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P271: 仅在室外或通风良好的地方使用。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

P403+P233: 存放在通风良好的地方。保持容器密闭。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P337+P317: 如果眼睛刺激持续:寻求医疗帮助。

P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。

P319: 如果你感到不适,请寻求医疗帮助。

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本产品的 CAS 号为 2627-69-2,分子式为 C9H14N4O5,分子量为 258.23 g/mol。
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