2. Cytoskeleton
  3. Myosin
  4. Omecamtiv mecarbil

Omecamtiv mecarbil  (Synonyms: CK-1827452)

製品番号: HY-14233 純度: 99.83%
COA 取扱説明書 Technical Support

Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.

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CAS 番号 : 873697-71-3

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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 108 在庫あり
Solution
10 mM * 1 mL in DMSO USD 108 在庫あり
Solid
5 mg $99 在庫あり
10 mg $165 在庫あり
25 mg $275 在庫あり
50 mg $415 在庫あり
100 mg $600 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Omecamtiv mecarbil:

Omecamtiv mecarbil 関連抗体

Top Publications Citing Use of Products

    Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351.

    Representative current traces achieved in the control period, with the presence of Omecamtiv mecarbil (OM) (3-10 µM), and washout of Omecamtiv mecarbil (OM).

    Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351.

    Concentration-dependent relationship of Omecamtiv mecarbil (OM) (0.3-100 µM) on the transient (INa(T), red open circles) and late (INa(L), black filled squares) components of INa evoked by short membrane depolarization.

    Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351.

    Quasi steady state inactivation curve of INa(T) taken with (red open circles) or without the addition (black filled circles) of Omecamtiv mecarbil (OM) (10 µM).

    Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351.

    The relationship of the relative INa(T) versus the PT duration obtained without (black filled circles) or with (red open circles) the application of Omecamtiv mecarbil (OM) (10 µM).

    Omecamtiv mecarbil purchased from MedChemExpress. Usage Cited in: Biomedicines. 2023 May 3;11(5):1351.

    The relationship of the relative amplitude of INa versus the stimulus duration achieved without (black filled circles) and with (red open circles) the presence of Omecamtiv mecarbil (OM) (10 µM).

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    MLCK

    • 生物活性

    • 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

    Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.

    体外実験

    Omecamtiv mecarbil (10 μM) reduces the maximal ATPase (kcat) 4.5-fold and dramatically reduces the actin concentration at which ATPase is half-maximal (KATPase) 30-fold. The Omecamtiv mecarbil-induced inhibition of the actin-activated ATPase is evaluated in a concentration-dependent manner to determine the EC50 (0.52 ± 0.10 μM). Omecamtiv mecarbil does not change the overall actin affinity. Omecamtiv mecarbil traps a population of myosin heads in a weak actin affinity state with slow product release. Omecamtiv mecarbil can reduce the actin sliding velocity more than 100-fold in the in vitro motility assay[3].

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

    Omecamtiv mecarbil 関連抗体
    体内実験

    Omecamtiv mecarbil (100-1000 ng/mL) demonstrates concentration-dependent increases in FS in Sprague Dawley rats model. Omecamtiv mecarbil demonstrates good PK parameters in both rats (Sprague Dawley) and dogs (Beagle) with clearances of 22 and 7.2 mL/min/kg, volumes of 3.5 and 3.6 L/kg, and bioavailabilities (F%) of 100 and 80%, respectively[1]. Omecamtiv mecarbil does not affect the phosphorylation status of myofilament proteins in both WT and KO hearts as shown by the absence of significant differences between pre and post Omecamtiv mecarbil samples within WT and KO groups, or affect the force generation at maximal Ca2+ activation (pCa 4.5) in any of the groups. Omecamtiv mecarbil increases the responsiveness of the cardiac myofilaments to Ca2+ at submaximal Ca2+-activations[2].

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

    401.43

    分子式

    C20H24FN5O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1CCN(CC1)CC2=C(C(NC(NC3=CC=C(N=C3)C)=O)=CC=C2)F)OC
    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 : 20 mg/mL (49.82 mM; ultrasonic and warming and heat to 60°C; 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 2.4911 mL 12.4555 mL 24.9109 mL
    5 mM 0.4982 mL 2.4911 mL 4.9822 mL
    10 mM 0.2491 mL 1.2455 mL 2.4911 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

    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）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    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 (6.23 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 (6.23 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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.83%

    COA (244 KB) RP-HPLC (247 KB) MS (69 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, 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 2.4911 mL 12.4555 mL 24.9109 mL 62.2774 mL
    5 mM 0.4982 mL 2.4911 mL 4.9822 mL 12.4555 mL
    10 mM 0.2491 mL 1.2455 mL 2.4911 mL 6.2277 mL
    15 mM 0.1661 mL 0.8304 mL 1.6607 mL 4.1518 mL
    20 mM 0.1246 mL 0.6228 mL 1.2455 mL 3.1139 mL
    25 mM 0.0996 mL 0.4982 mL 0.9964 mL 2.4911 mL
    30 mM 0.0830 mL 0.4152 mL 0.8304 mL 2.0759 mL
    40 mM 0.0623 mL 0.3114 mL 0.6228 mL 1.5569 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Omecamtiv mecarbil Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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:

    Omecamtiv mecarbil873697-71-3CK-1827452CK1827452CK 1827452MyosinInhibitorinhibitorinhibit

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    製品名:
    Omecamtiv mecarbil
    製品番号:
    HY-14233
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