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  4. Ascomycin

Ascomycin  (Synonyms: アスコマイシン; Immunomycin; FR-900520; FK520)

製品番号: HY-13557 純度: 99.96%
COA 取扱説明書 Technical Support

Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research.

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CAS 番号 : 104987-12-4

容量 価格（税別） 在庫状況 数量
>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 72 在庫あり
Solution
10 mM * 1 mL in DMSO USD 72 在庫あり
Solid
10 mg $66 在庫あり
50 mg $79 在庫あり
100 mg $103 在庫あり
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カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of Ascomycin:

Ascomycin 関連抗体

Top Publications Citing Use of Products

    Ascomycin purchased from MedChemExpress. Usage Cited in: MBio. 2017 Oct 24;8(5). pii: e01752-17.  [Abstract]

    Deletion of the FKB1 gene of M. furfur confers resistance to FK506. Sensitivity of the M. furfur strain CBS 14141 to the calcineurin inhibitors FK506, Ascomycin, and Pimecrolimus.

    Parasite 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
    Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

    Antibiotic 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
    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

    • 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

    Ascomycin (Immunomycin; FR-900520; FK520) is an ethyl analog of Tacrolimus (FK506) with strong immunosuppressant properties. Ascomycin is also a macrocyclic polyketide antibiotic with multiple biological activities such as anti-malarial, anti-fungal and anti-spasmodic. Ascomycin prevents graft rejection and has potential for varying skin ailments research[1][2].

    IC50 & Target

    Plasmodium

     

    Cellular Effect
    Cell Line Type Value Description References
    Jurkat IC50
    0.205 nM
    Compound: 2, FK520
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
    		10.1039/C2MD20266B
    Murine T-cell line IC50
    0.69 nM
    Compound: 2
    Inhibition of proliferation of PMA and Ionomycin stimulated murine T cells
    Inhibition of proliferation of PMA and Ionomycin stimulated murine T cells
    		10.1016/0960-894X(95)00161-L
    T-cell IC50
    0.69 nM
    Compound: 3 (Ascomycin)
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
    		10.1016/S0960-894X(01)81248-8
    T-cell IC50
    0.69 nM
    Compound: 1
    In vitro immunosuppressive activity in murine splenic T cells
    In vitro immunosuppressive activity in murine splenic T cells
    		[PMID: 10450986]
    T-cell IC50
    0.69 nM
    Compound: 1
    Immunosuppressive activity was determined as the ability to inhibit T cell proliferation.
    Immunosuppressive activity was determined as the ability to inhibit T cell proliferation.
    		[PMID: 9873523]
    T-cell IC50
    0.69 nM
    Compound: 2 ; 2A, (L-683590)
    In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    		10.1016/S0960-894X(01)80265-1
    T-cell IC50
    0.69 nM
    Compound: 2, (L-683590)
    In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
    		10.1016/S0960-894X(01)80264-X
    T-cell IC50
    0.69 nM
    Compound: Ascomycin
    In vitro suppression of T-cell proliferation.
    In vitro suppression of T-cell proliferation.
    		10.1016/S0960-894X(97)00409-5
    体外実験

    Ascomycin (FR-900520) suppresses immune response in vitro with an IC50 value of 0.55 nM for mouse mixed lymphocyte reaction[1].
    Ascomycin is a powerful calcium-dependent serine/threonine protein phosphatase (calcineurin [CaN], protein phosphatase 2B) inhibitors. Its mechanism of action involves the formation of a molecular complex with the intracellular FK506-binding protein-12 (FKBP12), thereby acquiring the ability to interact with CaN and to interfere with the dephosphorylation of various substrates[3].

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

    Ascomycin 関連抗体
    体内実験

    Ascomycin (FR-900520; i.m.; 0.32-32 mg/kg; 5 days a week; for 2 weeks) clearly prolongs skin allograft survival in rats[1].

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

    Animal Model: WKA rats (8-10 weeks old) transplanted with F344 skin allografts[1]
    Dosage: 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg, 32 mg/kg
    Administration: i.m.; 5 days a week; for 2 weeks
    Result: Clearly prolonged skin allograft survival in rats
    分子量

    792.01

    分子式

    C43H69NO12
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O
    Structure Classification
    Initial Source

    Streptomyces tubercidicus
    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 : ≥ 39 mg/mL (49.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2626 mL 6.3131 mL 12.6261 mL
    5 mM 0.2525 mL 1.2626 mL 2.5252 mL
    10 mM 0.1263 mL 0.6313 mL 1.2626 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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    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

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (3.16 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (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.
    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (2.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    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: 99.96%

    COA (261 KB) HNMR (294 KB) RP-HPLC (243 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 1.2626 mL 6.3131 mL 12.6261 mL 31.5653 mL
    5 mM 0.2525 mL 1.2626 mL 2.5252 mL 6.3131 mL
    10 mM 0.1263 mL 0.6313 mL 1.2626 mL 3.1565 mL
    15 mM 0.0842 mL 0.4209 mL 0.8417 mL 2.1044 mL
    20 mM 0.0631 mL 0.3157 mL 0.6313 mL 1.5783 mL
    25 mM 0.0505 mL 0.2525 mL 0.5050 mL 1.2626 mL
    30 mM 0.0421 mL 0.2104 mL 0.4209 mL 1.0522 mL
    40 mM 0.0316 mL 0.1578 mL 0.3157 mL 0.7891 mL
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    Ascomycin 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 *
    = × ×

    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:

    Ascomycin104987-12-4Immunomycin FR-900520 FK520FR900520FR 900520FR-900520FK520FK 520FK-520FKBPParasiteFungalAntibioticFK506-binding proteinimmunosuppressantmacrolideanti-malarialanti-fungalanti-spasmodicFKBP12Inhibitorinhibitorinhibit

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    製品名:
    Ascomycin
    製品番号:
    HY-13557
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