1. Epigenetics PI3K/Akt/mTOR Autophagy Stem Cell/Wnt Metabolic Enzyme/Protease
  2. AMPK Autophagy YAP Mitophagy Endogenous Metabolite
  3. AICAR

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

目录号: HY-13417 纯度: 99.98%
COA 产品使用指南

AICAR (Acadesine) 是一种腺苷类似物,也是一种 AMPK 激活剂。AICAR 调节葡萄糖和脂质的代谢,并抑制促炎细胞因子和 iNOS 的产生。AICAR 也是一种自噬 (autophagy),YAPmitophagy 抑制剂。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

AICAR Chemical Structure

AICAR Chemical Structure

CAS No. : 2627-69-2

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

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100 mg ¥860
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200 mg ¥1300
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500 mg ¥3000
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Customer Review

Other Forms of AICAR:

MCE 顾客使用本产品发表的 144 篇科研文献

WB
RT-PCR

    AICAR purchased from MCE. Usage Cited in: Antioxid Redox Signal. 2023 Apr 13.  [Abstract]

    AICAR (0.5 mM; 12 h) significantly increases the expression of Mfn2 in BUMPT Cells.

    AICAR purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 1;9(5):515.  [Abstract]

    Protein expression levels of AMPKα, p-AMPKα-thr172, p-ACC-ser79, LC3, Beclin-1, ATG5 and ATG7 in WT MSCs or control CrispCas MSCs, or AMPKα DKO MSCs before and after treatment with FAC or AICAR.

    AICAR purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3723-3738.  [Abstract]

    The effect of AICAR on the expression of AMPK, p-AMPK, mTOR, p-mTOR, and autophagy-related protein by Western blot analysis.

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jul 16;9:761.  [Abstract]

    Epithelial cells from colon tissue are extracted from mice in each group (n=6-8 per group) and protein level of p-AMPK (Thr172) and AMPKα1/2 are measured by western blot.

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345.  [Abstract]

    AMP-activated protein kinase (AMPK) activation by AST blunts dysfunction of lipid metabolism and resistance in HepG2 cells. Representative bands of SREBP-1c nuclear protein and cytoplasmic proteins are visualized in the immunoblotting assay.

    AICAR purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 16;9:345.  [Abstract]

    AMP-activated protein kinase activation by AST inhibits the expression of sterol regulatory element binding protein-1c (SREBP-1c) and SREBP-1c related genes. AST promotes AMPKa1 mRNA expression, AMPKa2 mRNA expression, and suppresses the expression of SREBP-1c, and its downstream genes FAS, ACC1, and also AMPK downstream gene SCD1.

    AICAR purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Dec;233(12):9701-9715.  [Abstract]

    HUVECs are pretreated with Compound C (5, 10, or 20 μM) for 18 hr or AICAR (1, 2, or 4 mM) for 1 hr, and then exposed to LSS for 30 min.

    AICAR purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.  [Abstract]

    Cells are treated with AICAR and AICAR (A++, 10 μM) + Compound C (C++, 1 μM) for 24 h, after which western blot analysis is performed.

    AICAR purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.  [Abstract]

    MC3T3-E1 cells are treated with AICAR (10 μM) in the presence or absence of 3-MA (5 mM) or CQ (10 μM) for 24 h, after which western blot analysis is conducted.

    AICAR purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.  [Abstract]

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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[1][2].

    IC50 & Target[1]

    AMPK

     

    Autophagy

     

    Mitophagy

     

    Human Endogenous Metabolite

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CCRF-CEM IC50
    210 μM
    Compound: 13, AICA
    Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis
    Cytostatic activity against human CEM cells assessed as growth inhibition after 3 days by particle counting analysis
    [PMID: 24177359]
    HCT-116 EC50
    > 100 μM
    Compound: AICAR
    Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells incubated for 48 hrs by MTT assay
    [PMID: 36518704]
    HCT-116 EC50
    > 100 μM
    Compound: AICAR
    Cytotoxicity against human HCT-116 cells overexpressing human MDR1 incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells overexpressing human MDR1 incubated for 48 hrs by MTT assay
    [PMID: 36518704]
    HCT-116 EC50
    > 100 μM
    Compound: AICAR
    Cytotoxicity against human HCT-116 cells overexpressing human BCRP incubated for 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells overexpressing human BCRP incubated for 48 hrs by MTT assay
    [PMID: 36518704]
    HEK293 EC50
    > 100 μM
    Compound: AICAR
    Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay
    Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay
    [PMID: 36518704]
    HeLa IC50
    ≥ 250 μM
    Compound: 13, AICA
    Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis
    Cytostatic activity against thymidine kinase-deficient human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis
    [PMID: 24177359]
    HeLa IC50
    165 μM
    Compound: 13, AICA
    Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis
    Cytostatic activity against human HeLa cells assessed as growth inhibition after 3 days by particle counting analysis
    [PMID: 24177359]
    K562 IC50
    800 μM
    Compound: AICAR
    Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay
    Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay
    [PMID: 29655981]
    K562 IC50
    800 μM
    Compound: Aca
    Antileukemic activity against human K562 cells after 48 hrs by XTT assay
    Antileukemic activity against human K562 cells after 48 hrs by XTT assay
    [PMID: 28094938]
    K-562R IC50
    800 μM
    Compound: AICAR
    Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay
    Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay
    [PMID: 29655981]
    L1210 IC50
    ≥ 250 μM
    Compound: 13, AICA
    Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis
    Cytostatic activity against mouse L1210 cells assessed as growth inhibition after 2 days by particle counting analysis
    [PMID: 24177359]
    MDA-MB-231 IC50
    1000 μM
    Compound: AICAR
    Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay
    Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay
    [PMID: 28325600]
    MDA-MB-453 IC50
    1700 μM
    Compound: AICAR
    Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
    Antiproliferation activity against human MDA-MB-453 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
    [PMID: 32007387]
    RCC4 IC50
    250 μM
    Compound: AICAR
    Anticancer activity against human RCC4 cells after 48 hrs by XTT assay
    Anticancer activity against human RCC4 cells after 48 hrs by XTT assay
    [PMID: 28325600]
    SK-BR-3 IC50
    180 μM
    Compound: AICAR
    Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
    Antiproliferation activity against human SK-BR-3 cells assessed as reduction in cell viability measured after 4 days by Celltiter-glo luminescent cell viability assay
    [PMID: 32007387]
    体外研究
    (In Vitro)

    HepG2 细胞分别用不同浓度的 AICAR (0.1-1.0 mM) 处理 12、24 和 48 小时。0.25、0.5 和 1.0 mM AICAR 的 IR-β 表达水平在 48 h 时显著降低至对照的 50%、53% 和 46%[1]

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

    体内研究
    (In Vivo)

    向 14 周大的雄性瘦 (L;体重 31.3 g) 野生型 和 ob/ob (O;体重 59.6 g) 小鼠注射 0.5 mg AMP 激活激酶 (AMPK) 激活剂 AICAR (A)/g 每天或盐水对照 (C) 14 天。最后一次注射后 24 小时 (包括禁食 12 小时),处死所有小鼠,切除跖屈肌复合体 (腓肠肌、比目鱼肌和跖肌) 进行分析。与体重变化无关,OC (159±12 mg) 小鼠的肌肉质量低于 LC、LA 和 OA (分别为 176±10、178±9 和 166±16 mg) 小鼠[3]
    与运动组和 AICAR (0.5 mg/g) 组相比,未处理组的肾脏重量明显更高。运动组的心脏重量高于其他组,而 AICAR 处理组的肝脏重量明显高于运动组和未处理组[4]

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

    Clinical Trial
    分子量

    258.23

    Formula

    C9H14N4O5

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    阿卡地新

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 116.67 mg/mL (451.81 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 65 mg/mL (251.71 mM; 超声加热助溶)

    配制储备液
    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
    查看完整工作液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    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

    • 方案 一

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

      Solubility: ≥ 5 mg/mL (19.36 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 5 mg/mL (19.36 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 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。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

    • 方案 一

      请依序添加每种溶剂: PBS

      Solubility: 110 mg/mL (425.98 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.98%

    参考文献
    Cell Assay
    [1]

    HepG2 cells (5×105 cells) are plated in 6-well culture plate dishes and then are incubated in the serum-free media for 12 h before transfection. One microgram of plasmid is transfected with FuGENE6 Transfection Reagent. After 5 h of transfection, the culture media are removed and then media supplemented with or without AICAR (0.1-1.0 mM) are added to each well. The stimulation media are changed every 24 h[1].

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

    Animal Administration
    [2][3]

    Mice[2]
    Fourteen-week-old lean (Lepob/+ or Lepob/+) and ob/ob (Lepob/Lepob) male mice are uesd. After the 14-day experimental treatment (24 h after AICAR injection, including a 12-h fast), the plantar flexor complex muscle is cleanly (tendon-to-tendon) excised from an anesthetized mouse. The muscle is quickly weighed and then processed for histology or frozen in liquid nitrogen and stored at -80°C. The anesthetized mice are killed by transection of the diaphragm and removal of the entire heart, after blood collection via needle puncture directly into the heart. AICAR or saline (control) is injected subcutaneously into the lateral distal portion of the back. AICAR is administered at 0.5 mg/g per day one time for 14 days. Saline (control) is injected in volumes identical to those used for AICAR treatment in a manner identical to that of AICAR treatment. Body weight is measured prior to death.
    Rats[3]
    Male 5-week-old ZDF rats are either subcutaneously injected with a single dose of AICAR (0.5 mg/g body wt) or underwent a single bout of treadmill running (60 min, speed of 25 m/min at a 5% incline). Untreated ZDF rats serve as controls (n=5 in each group). One hour after the subcutaneous AICAR injection or immediately after treadmill running, rats are killed by cervical dislocation. To avoid any effect of muscle spasm and hypoxia, red and white gastrocnemius muscles are removed within seconds and immediately freeze clamped for later determination of AMPK activity.

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

    参考文献

    完整工作液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 3.8725 mL 19.3626 mL 38.7252 mL 96.8129 mL
    5 mM 0.7745 mL 3.8725 mL 7.7450 mL 19.3626 mL
    10 mM 0.3873 mL 1.9363 mL 3.8725 mL 9.6813 mL
    15 mM 0.2582 mL 1.2908 mL 2.5817 mL 6.4542 mL
    20 mM 0.1936 mL 0.9681 mL 1.9363 mL 4.8406 mL
    25 mM 0.1549 mL 0.7745 mL 1.5490 mL 3.8725 mL
    30 mM 0.1291 mL 0.6454 mL 1.2908 mL 3.2271 mL
    40 mM 0.0968 mL 0.4841 mL 0.9681 mL 2.4203 mL
    50 mM 0.0775 mL 0.3873 mL 0.7745 mL 1.9363 mL
    60 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6135 mL
    80 mM 0.0484 mL 0.2420 mL 0.4841 mL 1.2102 mL
    100 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9681 mL

    * 该产品常见使用浓度在 mM 级别;建议您称取所需的量,然后将其溶解在培养基中,并用 0.22 μm 过滤器除菌,现用现配。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    AICAR
    目录号:
    HY-13417
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