2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Edelinontrine

Edelinontrine  (Synonyms: PF-04447943)

目录号: HY-15441 纯度: 99.85%
COA 产品使用指南

摩尔计算器

Edelinontrine (PF-04447943) 是一种有效的人重组 PDE9A 抑制剂，IC50 为 12 nM，比作用于其他PDE家族成员选择性高 78 倍 (IC50>1000 nM)。

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Edelinontrine Chemical Structure

Edelinontrine Chemical Structure

CAS No. : 1082744-20-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥960
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5 mg ￥873
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10 mg ￥1396
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25 mg ￥2790
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50 mg ￥4322
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100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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Customer Review

Edelinontrine 相关抗体

Top Publications Citing Use of Products

    Edelinontrine purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2017 Sep;38(9):1257-1268.  [Abstract]

    C33(S) can alleviate cardiac hypertrophic responses in vitro. Cardiomyocytes are pre-incubated by C33(S) and PF-7943 for 1 h followed by PE treatment or not. The protein levels of fetal genes are measured. C33(500): C33(S) 500 nM, C33(50): C33(S) 50 nM, PF-7943(2): PF-7943 (2 μM).

    查看 Phosphodiesterase (PDE) 亚型特异性产品:

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    PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM).

    IC50 & Target

    PDE9

     

    体外研究
    (In Vitro)

    Using recombinant human, rhesus, and rat PDE9A2 in a cell free assay Edelinontrine is shown to have a Ki of 2.8±0.26, 4.5±0.13, and 18.1±1.9 nM (n=4, 11 and 9 respectively). Edelinontrine is found to be highly selective over other PDE enzymes (PDE1, Ki=8600±2121 nM, n = 5; PDE2A3, Ki>99,000 nM; PDE3A, Ki>50,000 nM; PDE4A, Ki>29,000 nM; PDE5A, Ki=14,980±5025 nM, n=5; PDE6C, Ki=5324±2612 nM, n=4; PDE7A2, Ki>75,000 nM; PDE8A, Ki>50,000 nM; PDE10, Ki>51,250±20,056 nM, n=4; PDE11, Ki>80,000 nM) and no other significant activity at ~60 other receptors/enzymes. In HEK whole cells expressing rhesus PDE9A2, Edelinontrine inhibits ANP (0.3 μM) stimulated cGMP with an IC50 of 375±36.9 nM (n=16)[2].

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

    Edelinontrine 相关抗体:
    体内研究
    (In Vivo)

    Based on i.v. and p.o. dosing, pharmacokinetic studies with Edelinontrine in the rat indicates a Tmax of 0.3 h, T1/2 of 4.9 h, Cl of 21.7 mL/min/kg and an oral bioavailability of 47%. Thirty minutes following oral administration in rats (1-30 mg/kg), Edelinontrine concentrations dose-dependently increase in blood, brain and cerebrospinal fluid (CSF). The brain:plasma exposure ratios 30 min after dosing range from 0.13 at the 1 mg/kg dose to 0.33 at the 30 mg/kg dose. CSF levels are approximately 50% of brain levels. In mice, Edelinontrine (3, 10, 30 mg/kg p.o.) dose-dependently increases plasma and brain concentrations of Edelinontrine while the brain to plasma ratio ranged from 0.26 to 0.7 although this is not entirely dose dependent. CSF cGMP levels increase in a dose-dependent manner from a basal level of 3 pmol/mL to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels also increase in a dose-dependent manner from a basal level of 3 pmol/mL in vehicle treated animals to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels are elevated at all doses tested with a maximal effect of 3.5 fold increase above controls at 30 mg/kg[2].

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

    395.46

    Formula

    C20H25N7O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 54.6 mg/mL (138.07 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" 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 2.5287 mL 12.6435 mL 25.2870 mL
    5 mM 0.5057 mL 2.5287 mL 5.0574 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.32 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.85%

    COA (290 KB) HNMR (257 KB) LCMS (101 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    The rhesus PDE9A2 construct is subcloned into a pcDNA3.3 TOPO vector and HEK 293 cells, stably transfected to constitutively express rhesus PDE9A2 and hNPR1, are incubated with PF-04447943 (30 μM to 1.5 nM) in assay media at a density of 10,000 cells/well, for 30 min at 37°C. Cyclic GMP formation is stimulated by incubation with 0.3 μM ANP (Atrial Natriuretic Peptide) for another 30 min at 37°C. Following incubation, cells are lysed with Antibody/Lysis buffer and ED Reagent for 1 h at room temperature. After a subsequent incubation with EA Reagent for 30 min at room temperature, followed by incubation with Substrate Reagent for 1 h at room temperature, cGMP concentrations are determined by measuring luminescence on the Envision Microplate Luminometer. The maximal inhibition (100% activity) in the cell based assay is determined using 30 μM PF-04447943 and 0% activity is defined by the DMSO control. PF-04447943 is titrated in quadruplicate, in a 10 point titration. Percentage inhibition is calculated using the maximal inhibition value and IC50 values are calculated from concentration response curves using Prism software[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice and Rats[2]
    For the mouse studies, male C57Bl/6J mice are administered PF-04447943 (3, 10, 30 mg/kg p.o.). For the rat studies rats (strain, weight range and supplier as described in the novel object recognition study below) are administered PF-04447943 10 mg/kg i.v. and p.o.. At various times after administration the animals are anesthetized with isoflurane; blood samples are withdrawn via cardiac puncture and placed in EDTA tubes on ice. Plasma is separated and frozen at -70°C until assayed for drug concentration. PF-04447943 and the internal standard are monitored in the positive ion mode at the transition from m/z 396.2 to 203.1 and m/z 477.3 to 266.2, respectively. Quantification is performed using Analyst 1.4 based on duplicate standard curves.

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

    Edelinontrine 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5287 mL 12.6435 mL 25.2870 mL 63.2175 mL
    5 mM 0.5057 mL 2.5287 mL 5.0574 mL 12.6435 mL
    10 mM 0.2529 mL 1.2644 mL 2.5287 mL 6.3218 mL
    15 mM 0.1686 mL 0.8429 mL 1.6858 mL 4.2145 mL
    20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1609 mL
    25 mM 0.1011 mL 0.5057 mL 1.0115 mL 2.5287 mL
    30 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
    40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5804 mL
    50 mM 0.0506 mL 0.2529 mL 0.5057 mL 1.2644 mL
    60 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0536 mL
    80 mM 0.0316 mL 0.1580 mL 0.3161 mL 0.7902 mL
    100 mM 0.0253 mL 0.1264 mL 0.2529 mL 0.6322 mL
    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:

    Edelinontrine1082744-20-4PF-04447943PF04447943PF 04447943Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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