2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Senicapoc

Senicapoc  (Synonyms: ICA-17043)

製品番号: HY-50694 純度: 99.91%
COA 取扱説明書 Technical Support

Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.

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CAS 番号 : 289656-45-7

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 59 在庫あり
Solution
10 mM * 1 mL in DMSO USD 59 在庫あり
Solid
5 mg $54 在庫あり
10 mg $73 在庫あり
25 mg $118 在庫あり
50 mg $153 在庫あり
100 mg $200 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of Senicapoc:

Senicapoc 関連抗体

Top Publications Citing Use of Products

    Senicapoc purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2017 Jan 15:795:1-7.  [Abstract]

    In a second cohort of rats, the 50% paw withdrawal threshold (g) in response to von Frey stimulation of the injured hind paw is determined in CCI rats (n=12/group) dosed with either vehicle, Senicapoc (SEN) or GBP. The efficacy of Senicapoc (10, 30 and 100 mg/kg, p.o.) is evaluated at its Tmax, 4 h after dosing.

    Senicapoc purchased from MedChemExpress. Usage Cited in: J Cancer. 2017 Jun 3;8(9):1568-1578.  [Abstract]

    H&E staining and Ki-67 immunohistochemistry of the respective tumors in two groups are performed.

    • 生物活性

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM[1].

    IC50 & Target

    IC50: 11 nM (Gardos channel)[1]
    体外実験

    ICA-17043 is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6 nM. ICA-17043 blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion[1].

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

    Senicapoc 関連抗体
    体内実験

    ICA-17043 (10 mg/kg, p.o.) administration produces a significant decrease in Gardos channel activity measured at day 11 and 21 and is associated with a corresponding increase in red cell K+ content without changes in Na+ content. ICA-17043 (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse[1]. Senicapoc (30 mg/kg, p.o.) reduces airway hyperresponsiveness, eosinophil numbers in bronchoalveolar lavage taken 48 hours post-allergen challenge, and vascular remodelling in the sheep[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    323.34

    分子式

    C20H15F2NO
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(C(C1=CC=CC=C1)(C2=CC=C(C=C2)F)C3=CC=C(F)C=C3)N
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (154.64 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 3.0927 mL 15.4636 mL 30.9272 mL
    5 mM 0.6185 mL 3.0927 mL 6.1854 mL
    10 mM 0.3093 mL 1.5464 mL 3.0927 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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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    体内:

    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: ≥ 2.5 mg/mL (7.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.91%

    COA (249 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [1]

    The whole blood is initially diluted 1:1 with Modified Flux Buffer (MFB), consisting of 140 mM NaCl, 5 mM KCl, 10 mM Tris (tris(hydroxymethyl)aminomethane), 0.1 mM EGTA (ethyleneglycoltetraacetic acid) (pH=7.4). The blood is centrifuged at 1000 rpm, and the pellet comprised primarily of RBCs is washed 3 times with MFB. The cells are then loaded with 86Rb+ by incubating the washed cells with 86Rb+ at a final concentration of 0.185 MBq/mL (5 μCi/mL) in MFB for at least 3 hours at 37°C. After loading with 86Rb+, the RBCs are washed 3 times with chilled MFB. The cells are then incubated for 10 minutes with test compound (senicapoc) at concentrations that ranged from 1 nM to 10 000 nM. Efflux of 86Rb+ is initiated by raising intracellular calcium levels in the RBCs with the addition of CaCl2 and A23187 (a calcium ionophore) to final concentrations of 2 mM and 5 μM, respectively. After 10 minutes of incubation at room temperature, the RBCs are pelleted in a microcentrifuge, and the supernatant is removed and counted in a Wallac MicroBeta liquid scintillation counter.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Transgenic Hbbsingle/single SAD1 (SAD) female and male mice between 3 and 6 months of age, weighing 25 to 30 g, are used for this study. The SAD mice are divided into 2 groups, and either vehicle (n=6) or senicapoc (10 mg/kg) (n=6) is administered orally by gavage twice daily. C57B6/2J mice are used as controls (wild-type mice). Hematologic parameters are evaluated at baseline and after 11 and 21 days of therapy. Blood sampling and vehicle administration have previously been shown not to affect the blood parameters measured in this study.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0927 mL 15.4636 mL 30.9272 mL 77.3180 mL
    5 mM 0.6185 mL 3.0927 mL 6.1854 mL 15.4636 mL
    10 mM 0.3093 mL 1.5464 mL 3.0927 mL 7.7318 mL
    15 mM 0.2062 mL 1.0309 mL 2.0618 mL 5.1545 mL
    20 mM 0.1546 mL 0.7732 mL 1.5464 mL 3.8659 mL
    25 mM 0.1237 mL 0.6185 mL 1.2371 mL 3.0927 mL
    30 mM 0.1031 mL 0.5155 mL 1.0309 mL 2.5773 mL
    40 mM 0.0773 mL 0.3866 mL 0.7732 mL 1.9329 mL
    50 mM 0.0619 mL 0.3093 mL 0.6185 mL 1.5464 mL
    60 mM 0.0515 mL 0.2577 mL 0.5155 mL 1.2886 mL
    80 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9665 mL
    100 mM 0.0309 mL 0.1546 mL 0.3093 mL 0.7732 mL
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    Senicapoc Related Classifications

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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）
    × = ×
    C1   V1   C2   V2
    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:

    Senicapoc289656-45-7ICA-17043ICA17043ICA 17043Potassium ChannelKcsAInhibitorinhibitorinhibit

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    製品番号:
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