2. Metabolic Enzyme/Protease Apoptosis
  3. HIF/HIF Prolyl-Hydroxylase Ferroptosis
  4. Roxadustat

Roxadustat  (Synonyms: FG-4592)

製品番号: HY-13426 純度: 99.92%
COA 取扱説明書 Technical Support

Roxadustat is an orally active hypoxia-inducible factor prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 808118-40-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 41 在庫あり
Solution
10 mM * 1 mL in DMSO USD 41 在庫あり
Solid
5 mg $38 在庫あり
10 mg $60 在庫あり
25 mg $85 在庫あり
50 mg $108 在庫あり
100 mg $144 在庫あり
200 mg $228 在庫あり
500 mg $348 在庫あり
1 g $540 在庫あり
5 g   お問い合わせ  
10 g   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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 59 publication(s) in Google Scholar

Other Forms of Roxadustat:

Roxadustat 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
IF

    Roxadustat purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Jan;23(1):349-356.  [Abstract]

    FG-4592 increases level of HIF-1α and regulates apoptosis-related proteins in AHH-1. The effects of FG-4592 on HIF1-α are detected using Western Blot. Level of HIF-1α is measured at different time points after the treatment of FG-4592 (A). Cell lysate is obtained at 6 h after irradiation and used to evaluate the regulation of FG-4592 on apoptosis-related molecules. Apoptosis promoting molecules (c-caspase3 and cyt-c) are downregulated and molecules that inhibit apoptosis are up-regulated by FG-4

    Roxadustat purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2019 Jan;23(1):349-356.  [Abstract]

    FG-4592 mitigates radiation-induced DNA injuries. AHH-1 cells pretreated with or without FG-4592 are exposed to 6 Gy irradiation and γ-H2AX assay is used to determine DNA damages at 0, 0.5, 2 h after irradiation.

    Roxadustat purchased from MedChemExpress. Usage Cited in: Science. 2016 Apr 1;352(6281):54-61.  [Abstract]

    FG-4592 causes normoxic stabilization of HIF1α and rewires energy metabolism. Immunoblot showing HIF1α ± RC inhibition with antimycin or oligomycin, ± FG-4592 under normoxia (21% O2) or hypoxia (1% O2). RC inhibition prevents HIF1α stabilization during hypoxia. FG-4592 administration overcomes this paradox and stabilizes HIF1α even during normoxia. Immunoblot is representative of independent experiments done in duplicate in HT-29 cells.

    HIF/HIF Prolyl-Hydroxylase 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
    HIF-1α HIF

    • 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

    Roxadustat is an orally active hypoxia-inducible factor prolyl-hydroxylase (PHD) inhibitor (HIF-PHI) that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin[1].

    IC50 & Target

    Hypoxia-inducible factor prolyl-hydroxylase[1]
    Cellular Effect
    Cell Line Type Value Description References
    HK-2 IC50
    0.01 μM
    Compound: 153
    Downregulation of BNIP3 expression in human HK-2 cells incubated for 6 hrs by Western blot analysis
    Downregulation of BNIP3 expression in human HK-2 cells incubated for 6 hrs by Western blot analysis
    		[PMID: 38295689]
    体外実験

    Roxadustat (5-50 μM; 6 hours) significantly inhibits TBHP-induced apoptosis in PC12 cells[2].
    Roxadustat (50 μM; 6 hours) stabilizes HIF-1α protein expression in PC12 cells[2].

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

    Roxadustat 関連抗体

    Apoptosis Analysis[2]

    Cell Line: PC12 cells
    Concentration: 5, 20, 50 μM
    Incubation Time: 6 hours
    Result: Significantly inhibited TBHP-induced apoptosis.

    Western Blot Analysis[2]

    Cell Line: PC12 cells
    Concentration: 50 μM
    Incubation Time: 6 hours
    Result: stabilized HIF-1α protein expression.
    体内実験

    Roxadustat (50 mg/kg; i.p.; daily for 7 days) protects the survival of motor neurons and improves recovery from spinal cord injury[2].

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

    Animal Model: 12-week female C57BL/6 mice[2]
    Dosage: 50 mg/kg
    Administration: Intraperitoneal injection; daily for 7 days
    Result: Protected the survival of motor neurons and improved recovery from spinal cord injury.
    臨床実験
    分子量

    352.34

    分子式

    C19H16N2O5
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(O)CNC(C1=C(O)C2=C(C(C)=N1)C=C(OC3=CC=CC=C3)C=C2)=O
    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 : 100 mg/mL (283.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8382 mL 14.1908 mL 28.3817 mL
    5 mM 0.5676 mL 2.8382 mL 5.6763 mL
    10 mM 0.2838 mL 1.4191 mL 2.8382 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.10 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 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:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (14.19 mM); Suspended solution; Need ultrasonic

    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: 99.92%

    COA (245 KB) LCMS (95 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8382 mL 14.1908 mL 28.3817 mL 70.9542 mL
    5 mM 0.5676 mL 2.8382 mL 5.6763 mL 14.1908 mL
    10 mM 0.2838 mL 1.4191 mL 2.8382 mL 7.0954 mL
    15 mM 0.1892 mL 0.9461 mL 1.8921 mL 4.7303 mL
    20 mM 0.1419 mL 0.7095 mL 1.4191 mL 3.5477 mL
    25 mM 0.1135 mL 0.5676 mL 1.1353 mL 2.8382 mL
    30 mM 0.0946 mL 0.4730 mL 0.9461 mL 2.3651 mL
    40 mM 0.0710 mL 0.3548 mL 0.7095 mL 1.7739 mL
    50 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4191 mL
    60 mM 0.0473 mL 0.2365 mL 0.4730 mL 1.1826 mL
    80 mM 0.0355 mL 0.1774 mL 0.3548 mL 0.8869 mL
    100 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7095 mL
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    Roxadustat 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:

    Roxadustat808118-40-3FG-4592FG4592FG 4592HIF/HIF Prolyl-HydroxylaseFerroptosisHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
    HY-13426
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