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  3. PRE-084 hydrochloride

PRE-084 hydrochloride 

目录号: HY-18100A 纯度: 99.92%
COA 产品使用指南

PRE-084 hydrochloride 是一种高选择性的σ1 受体 (S1R) 激动剂,其 IC50 值为 44 nM。PRE-084 hydrochloride 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 hydrochloride 还能通过激活 Akt-eNOS 途径来改善大鼠心肌缺血再灌注损伤。

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PRE-084 hydrochloride Chemical Structure

PRE-084 hydrochloride Chemical Structure

CAS No. : 75136-54-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥830
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5 mg ¥468
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10 mg ¥750
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50 mg ¥3000
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100 mg ¥5500
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200 mg 现货 询价
500 mg   询价  
1 g   询价  

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Customer Review

Other Forms of PRE-084 hydrochloride:

    PRE-084 hydrochloride 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 hydrochloride 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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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

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

    IC50 & Target

    eNOS

     

    Sigma 1 Receptor

     

    体外研究
    (In Vitro)

    PRE-084 hydrochloride (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.

    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 hydrochloride (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 hydrochloride (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.
    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

    353.88

    Formula

    C19H28ClNO3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    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
    细胞实验: 

    H2O 中的溶解度 : 33.33 mg/mL (94.18 mM; 超声助溶 (<60°C))

    DMSO 中的溶解度 : 17.5 mg/mL (49.45 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.8258 mL 14.1291 mL 28.2582 mL
    5 mM 0.5652 mL 2.8258 mL 5.6516 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

    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: ≥ 2.08 mg/mL (5.88 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.88 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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。
    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: 99.92%

    参考文献

    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
    DMSO / H2O 1 mM 2.8258 mL 14.1291 mL 28.2582 mL 70.6454 mL
    5 mM 0.5652 mL 2.8258 mL 5.6516 mL 14.1291 mL
    10 mM 0.2826 mL 1.4129 mL 2.8258 mL 7.0645 mL
    15 mM 0.1884 mL 0.9419 mL 1.8839 mL 4.7097 mL
    20 mM 0.1413 mL 0.7065 mL 1.4129 mL 3.5323 mL
    25 mM 0.1130 mL 0.5652 mL 1.1303 mL 2.8258 mL
    30 mM 0.0942 mL 0.4710 mL 0.9419 mL 2.3548 mL
    40 mM 0.0706 mL 0.3532 mL 0.7065 mL 1.7661 mL
    H2O 50 mM 0.0565 mL 0.2826 mL 0.5652 mL 1.4129 mL
    60 mM 0.0471 mL 0.2355 mL 0.4710 mL 1.1774 mL
    80 mM 0.0353 mL 0.1766 mL 0.3532 mL 0.8831 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.

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    产品名称:
    PRE-084 hydrochloride
    目录号:
    HY-18100A
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