2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. PNU-282987

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.

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CAS 番号 : 123464-89-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $79 在庫あり
25 mg $160 在庫あり
50 mg $288 在庫あり
100 mg $410 在庫あり
200 mg   お問い合わせ  
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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

Other Forms of PNU-282987:

PNU 282987 関連抗体

Top Publications Citing Use of Products

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) reduced Nlrp3 mRNA level in the oxygen-glucose deprivation/reperfusion (OGD/R) model performed in BV2 cells.

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) diminished the upregulation of NLRP3 expression induced by LPS + ATP in BV2 cells.

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) blocked conspicuous nucleus translocation by LPS + ATP stimulation in BV2 cells.

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) reduced the release of IL-1β in the conditioned medium collected from BV2 cells.

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    PNU-282987 (0.1 μM; 1 h) significantly ameliorated the apoptosis of PC12 cells induced by the LPS + ATP-containing conditioned medium.

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Apr;72(4):879-892.  [Abstract]

    PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.

    5-HT Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems[1].

    IC50 & Target

    IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA)[1]
    体外実験

    PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM[1].
    PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM[1].
    PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM[1].

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

    PNU 282987 関連抗体
    体内実験

    PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit[1].
    PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner[1].

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

    Animal Model: Rats[1]
    Dosage: 1, 3 mg/kg
    Administration: i.v.
    Result: Significantly reversed amphetamine-induced gating deficit.
    分子量

    301.21

    分子式

    C14H18Cl2N2O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=C(C=C1)Cl)N[C@H]2CN3CCC2CC3.[H]Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

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

    H2O : 50 mg/mL (166.00 mM; Need ultrasonic)

    DMSO : 17.5 mg/mL (58.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3199 mL 16.5997 mL 33.1994 mL
    5 mM 0.6640 mL 3.3199 mL 6.6399 mL
    10 mM 0.3320 mL 1.6600 mL 3.3199 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1 mg/mL (3.32 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1 mg/mL (3.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (166.00 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    g

    Dosing volume
    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.93%

    COA (249 KB) HNMR (249 KB) RP-HPLC (245 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 3.3199 mL 16.5997 mL 33.1994 mL 82.9986 mL
    5 mM 0.6640 mL 3.3199 mL 6.6399 mL 16.5997 mL
    10 mM 0.3320 mL 1.6600 mL 3.3199 mL 8.2999 mL
    15 mM 0.2213 mL 1.1066 mL 2.2133 mL 5.5332 mL
    20 mM 0.1660 mL 0.8300 mL 1.6600 mL 4.1499 mL
    25 mM 0.1328 mL 0.6640 mL 1.3280 mL 3.3199 mL
    30 mM 0.1107 mL 0.5533 mL 1.1066 mL 2.7666 mL
    40 mM 0.0830 mL 0.4150 mL 0.8300 mL 2.0750 mL
    50 mM 0.0664 mL 0.3320 mL 0.6640 mL 1.6600 mL
    H2O 60 mM 0.0553 mL 0.2767 mL 0.5533 mL 1.3833 mL
    80 mM 0.0415 mL 0.2075 mL 0.4150 mL 1.0375 mL
    100 mM 0.0332 mL 0.1660 mL 0.3320 mL 0.8300 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    PNU-282987 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • 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:

    PNU-282987123464-89-1PNU282987PNU 282987nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptornicotinic acetylcholine receptors (nAChRs)5-HT3nervous systemsα7Inhibitorinhibitorinhibit

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    製品番号:
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