2. Neuronal Signaling PI3K/Akt/mTOR Immunology/Inflammation
  3. Sigma Receptor Akt NO Synthase
  4. PRE-084

PRE-084 是一种高选择性的 σ1 受体 (S1R) 激动剂，其 IC50 值为 44 nM。PRE-084 具有较好的神经保护作用，可改善小鼠的运动功能和运动神经元的存活率。PRE-084 还能通过激活 Akt-eNOS 途径来改善大鼠心肌缺血再灌注损伤。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 PRE-084 hydrochloride 通常具有更好的水溶性和稳定性。

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PRE-084 Chemical Structure

PRE-084 Chemical Structure

CAS No. : 138847-85-5

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PRE-084 的其他形式现货产品:

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PRE-084 相关抗体

Top Publications Citing Use of Products

    PRE-084 purchased from MCE. Usage Cited in: Exp Neurol. 2022 Mar 5;114034.  [Abstract]

    The therapeutic effect of the σ-1R agonist PRE-084 (0.6 mg/kg; i.p.) in SPS rats is blocked by the mTOR signaling pathway inhibitor Rapamycin.

    PRE-084 purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507.  [Abstract]

    Chronic PRE-084 treatment alleviates DA neuron loss in Dicer cKO mice. TH and Iba1 immunostaining. Representative photomicrographs are shown at ×20 magnification (scale bars, 100 μm).

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    nNOS iNOS eNOS

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].

    体外研究
    (In Vitro)

    PRE-084 (0.1-100 µM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 µM) and reduces the levels of proapoptotic protein Bax at 10 µM[1].

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

    PRE-084 相关抗体:

    Cell Viability Assay[1]

    Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model)
    Concentration: 0.1-100 µM
    Incubation Time: 24 h
    Result: Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM.

    Western Blot Analysis[1]

    Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model)
    Concentration: 10 µM
    Incubation Time: 24 h
    Result: Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).
    体内研究
    (In Vivo)

    PRE-084 (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)[2].
    PRE-084 (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model[3].

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

    Animal Model: Wobbler mice (4-week-old)[2].
    Dosage: 0.25 mg/kg
    Administration: Intraperitoneal injection; 3 times a week for 8 weeks.
    Result: Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.
    Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.
    Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons.
    Animal Model: Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)[3].
    Dosage: 1 mg/kg
    Administration: Intraperitoneal injection; single.
    Result: Significantly decreased the degree of myocardial apoptosis.
    Led to significantly increased expression of p‑Akt and p‑eNOS.
    分子量

    317.42

    Formula

    C19H27NO3
    CAS 号
    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

    PRE-084 相关分类

    • 摩尔计算器

    • 稀释计算器

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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:

    PRE-084138847-85-5PRE084PRE 084Sigma ReceptorAktNO SynthasePKBProtein kinase BNitric oxide synthasesNOSneurological diseasesneuroprotectionAlzheimer’s diseaseALSMIcortical cells；2023年2月竞品,张林曦要求上线20230414；https://sci-hub.se/10.1016/j.jneuroim.2003.10.020Inhibitorinhibitorinhibit

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    目录号：
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