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

Aliskiren hydrochloride  (Synonyms: CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride)

目录号: HY-12176A
产品使用指南

摩尔计算器

Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride 是一种口服有效的、选择性的肾素 (renin) 抑制剂，IC50 为 1.5 nM。Aliskiren hydrochloride 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 hydrochloride Chemical Structure

Aliskiren hydrochloride Chemical Structure

CAS No. : 173399-03-6

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Aliskiren hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of Aliskiren hydrochloride:

Aliskiren hydrochloride 相关抗体

Top Publications Citing Use of Products

    Aliskiren hydrochloride 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 hydrochloride 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) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1]-[4].

    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 hydrochloride inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
    Aliskiren hydrochloride (10 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
    Aliskiren hydrochloride (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 hydrochloride 相关抗体:

    Cell Migration 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 hydrochloride (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 hydrochloride (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 hydrochloride (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

    588.22

    Formula

    C30H54ClN3O6
    CAS 号
    中文名称

    盐酸阿利克仑半富马酸盐 d6
    运输条件

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

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Aliskiren hydrochloride 相关分类

    • 摩尔计算器

    • 稀释计算器

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    The dilution calculator equation

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    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:

    Aliskiren173399-03-6CGP 60536CGP60536BSPP 100盐酸阿利克仑半富马酸盐 d6CGP60536CGP-60536SPP100SPP-100ReninAutophagyHypertensioncardiovascular diseasescancercachexiaC26colon carcinomaInhibitorinhibitorinhibit

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    目录号：
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