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  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)

目錄號: HY-13417 純度: 99.98%
COA 產(chǎn)品使用指南

AICAR (Acadesine) 是一種腺苷類似物,也是一種 AMPK 激活劑。AICAR 調(diào)節(jié)葡萄糖和脂質(zhì)的代謝,并抑制促炎細(xì)胞因子和 iNOS 的產(chǎn)生。AICAR 也是一種自噬 (autophagy),YAPmitophagy 抑制劑。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個人用途提供產(chǎn)品和服務(wù)

AICAR Chemical Structure

AICAR Chemical Structure

CAS No. : 2627-69-2

1.  客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2.  同一機(jī)構(gòu)(單位)同一產(chǎn)品試用裝僅限申領(lǐng)一次,同一機(jī)構(gòu)(單位)一年內(nèi)

     可免費(fèi)申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
50 mg ¥520
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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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1 g ¥5100
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Customer Review

Other Forms of AICAR:

MCE 顧客使用本產(chǎn)品發(fā)表的 145 篇科研文獻(xiàn)

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

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    細(xì)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]
    體外研究
    (In Vitro)

    HepG2 細(xì)胞分別用不同濃度的 AICAR (0.1-1.0 mM) 處理 12、24 和 48 小時。0.25、0.5 和 1.0 mM AICAR 的 IR-β 表達(dá)水平在 48 h 時顯著降低至對照的 50%、53% 和 46%[1]

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

    體內(nèi)研究
    (In Vivo)

    向 14 周大的雄性瘦 (L;體重 31.3 g) 野生型 和 ob/ob (O;體重 59.6 g) 小鼠注射 0.5 mg AMP 激活激酶 (AMPK) 激活劑 AICAR (A)/g 每天或鹽水對照 (C) 14 天。最后一次注射后 24 小時 (包括禁食 12 小時),處死所有小鼠,切除跖屈肌復(fù)合體 (腓腸肌、比目魚肌和跖肌) 進(jìn)行分析。與體重變化無關(guān),OC (159±12 mg) 小鼠的肌肉質(zhì)量低于 LC、LA 和 OA (分別為 176±10、178±9 和 166±16 mg) 小鼠[3]。
    與運(yùn)動組和 AICAR (0.5 mg/g) 組相比,未處理組的腎臟重量明顯更高。運(yùn)動組的心臟重量高于其他組,而 AICAR 處理組的肝臟重量明顯高于運(yùn)動組和未處理組[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 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    阿卡地新

    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 116.67 mg/mL (451.81 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

    H2O 中的溶解度 : 65 mg/mL (251.71 mM; 超聲加熱助溶)

    配制儲備液
    濃度 溶劑體積 質(zhì)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

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實(shí)驗(yàn):

    請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可獲得 ≥ 5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可獲得 ≥ 5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

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

    以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑: PBS

      Solubility: 110 mg/mL (425.98 mM); 澄清溶液; 超聲助溶

    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳,請具體參考實(shí)測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.98%

    參考文獻(xiàn)
    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.

    參考文獻(xiàn)

    完整工作液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
    儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請?jiān)?年內(nèi)使用, -20°C儲存時,請?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 該產(chǎn)品常見使用濃度在 mM 級別;建議您稱取所需的量,然后將其溶解在培養(yǎng)基中,并用 0.22 μm 過濾器除菌,現(xiàn)用現(xiàn)配。

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    • 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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    產(chǎn)品名稱:
    AICAR
    目錄號:
    HY-13417
    需求量: