2. Metabolic Enzyme/Protease Autophagy
  3. Renin Autophagy
  4. Aliskiren hemifumarate

Aliskiren hemifumarate  (Synonyms: 阿利克仑半富马酸盐; CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate)

目录号: HY-12177 纯度: 99.80%
COA 产品使用指南

摩尔计算器

Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate 是一种口服有效的、选择性的肾素 (renin) 抑制剂，IC50 为 1.5 nM。Aliskiren hemifumarate 可用于高血压、心血管疾病和癌症恶病质的研究。

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Aliskiren hemifumarate Chemical Structure

Aliskiren hemifumarate Chemical Structure

CAS No. : 173334-58-2

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥698
In-stock
5 mg ￥325
In-stock
10 mg ￥520
In-stock
50 mg ￥1100
In-stock
100 mg ￥1800
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Aliskiren hemifumarate:

Aliskiren hemifumarate 相关抗体

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Top Publications Citing Use of Products

    Aliskiren hemifumarate purchased from MCE. Usage Cited in: Lipids Health Dis. 2018 Jul 31;17(1):183.  [Abstract]

    Protein abundance of ER stress markers (BiP, IRE1α, PERK, ATF4, pS51-eIF2α, eIF2α, and CHOP) are upregulated after palmitic acid (PA) treatment, which is prevented by cotreatment with chymostatin (50μM) and Aliskiren (10 nM).

    Aliskiren hemifumarate purchased from MCE. Usage Cited in: Department of Biological Science. National Sun Yat-Sen University. 2015 Sep.

    Effects of Aliskiren (AK) produce efficacious antagonism of the protein expression of c-Fos (A), GFAP (B) and OX-42 (C) in SC, aCSF+MCAO, AK+MCAO or AK alone group one day after stroke.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

    IC50 & Target

    IC50: 1.5 nM (renin)[1]; 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)[2]
    体外研究
    (In Vitro)

    Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
    Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
    Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2].

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

    Aliskiren hemifumarate 相关抗体:

    Cell Viability Assay[2]

    Cell Line: Smooth muscle cell (SMC)
    Concentration: 1-10 μM
    Incubation Time: 24 hours
    Result: Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.
    体内研究
    (In Vivo)

    Aliskiren hemifumarate (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets[3].
    Aliskiren hemifumarate (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole‑body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4].
    Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].

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

    Animal Model: Sodium-depleted marmosets[3]
    Dosage: 3 mg/kg, 10 mg/kg
    Administration: Oral gavage; once daily; 12 days
    Result: Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate.
    Showed no rebound increase in BP following the end of treatment with either dose of aliskiren.
    Inhibited the RAS and controls the upregulation of pro‑inflammatory cytokines.
    Animal Model: Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4]
    Dosage: 10 mg/kg
    Administration: Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
    Result: Enhanced grip strength, coordination, and locomotor activity.
    Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor‑α (TNF‑α) and inter‑ leukin‑6 (IL‑6) levels.
    Clinical Trial
    分子量

    1219.59

    Formula

    C64H110N6O16
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    阿利克仑半富马酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : ≥ 50 mg/mL (41.00 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 0.8199 mL 4.0997 mL 8.1995 mL
    5 mM 0.1640 mL 0.8199 mL 1.6399 mL
    查看完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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

    In Vivo:

    以下溶解方案，请直接配置工作液。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: 50 mg/mL (41.00 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

    只
    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
    参考文献

    Aliskiren hemifumarate 相关分类

    完整储备液配制表

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 0.8199 mL 4.0997 mL 8.1995 mL 20.4987 mL
    5 mM 0.1640 mL 0.8199 mL 1.6399 mL 4.0997 mL
    10 mM 0.0820 mL 0.4100 mL 0.8199 mL 2.0499 mL
    15 mM 0.0547 mL 0.2733 mL 0.5466 mL 1.3666 mL
    20 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0249 mL
    25 mM 0.0328 mL 0.1640 mL 0.3280 mL 0.8199 mL
    30 mM 0.0273 mL 0.1367 mL 0.2733 mL 0.6833 mL
    40 mM 0.0205 mL 0.1025 mL 0.2050 mL 0.5125 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    Keywords:

    Aliskiren hemifumarate173334-58-2CGP 60536 hemifumarateCGP60536B hemifumarateSPP 100 hemifumarate阿利克仑半富马酸盐ReninAutophagyHypertensioncardiovascular diseasescancercachexiaC26colon carcinomaInhibitorinhibitorinhibit

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