2. Membrane Transporter/Ion Channel
  3. SGLT
  4. Canagliflozin

Canagliflozin  (Synonyms: JNJ 28431754)

製品番号: HY-10451 純度: 99.99%
COA 取扱説明書 Technical Support

Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

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CAS 番号 : 842133-18-0

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 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
5 mg $55 在庫あり
10 mg $77 在庫あり
50 mg $121 在庫あり
100 mg $154 在庫あり
200 mg $218 在庫あり
500 mg $350 在庫あり
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カスタマーレビュー

Based on 46 publication(s) in Google Scholar

Other Forms of Canagliflozin:

Canagliflozin 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    Canagliflozin purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Dec;132:110821.  [Abstract]

    MCF-7 and ZR-75-1 cells are exposed to Canagliflozin 0, 11, 33, and 100 μM for 24 h and protein levels of p-AMPK, total AMPK, p-p70S6K1 and total p70S6K1 are detected using immunoblot assay.

    Canagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59.  [Abstract]

    Effects of NF-κB inhibitor (10 μM MLN120B) is measured on p62 protein in LPS-induced RAW264.7 cells.

    Canagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59.  [Abstract]

    PFK2 expression is significantly increased by LPS but is attenuated by Canagliflozin (CAN).

    SGLT 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
    SGLT1 SGLT2

    • 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

    Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively[1].

    IC50 & Target

    SGLT2

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 IC50
    1900 1
    Compound: 4
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    CHO-K1 IC50
    1900 1
    Compound: 4
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    CHO-K1 IC50
    6.7 1
    Compound: 4
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    CHO-K1 IC50
    1900 1
    Compound: 4
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    CHO-K1 IC50
    6.7 1
    Compound: 4
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    CHO-K1 IC50
    6.7 1
    Compound: 4
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay
    		[PMID: 22652255]
    体外実験

    Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1].

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

    Canagliflozin 関連抗体
    体内実験

    Canagliflozin (30 mg/kg treatment for 4 weeks) reduces blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice[1].
    Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats[1].

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

    Animal Model: Diet-induced obese, insulin resistantmice (DIO) Mice[1]
    Dosage: 30 mg/kg
    Administration: Oral gavage; daily; 4 weeks
    Result: Reduced BG levels, respiratory exchange ratio, and body weight gain.
    Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats[1]
    Dosage: 3 mg/kg
    Administration: Oral gavage; daily; 3 weeks
    Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.
    分子量

    444.52

    分子式

    C24H25FO5S
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC1=CC=C(C2=CC=C(CC3=C(C=CC([C@@H]4O[C@@H]([C@H]([C@@H]([C@H]4O)O)O)CO)=C3)C)S2)C=C1
    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 (112.48 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 2.2496 mL 11.2481 mL 22.4962 mL
    5 mM 0.4499 mL 2.2496 mL 4.4992 mL
    10 mM 0.2250 mL 1.1248 mL 2.2496 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)

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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）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (22.50 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
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    %
    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: 99.99%

    COA (247 KB) HNMR (297 KB) RP-HPLC (249 KB) LCMS (339 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 2.2496 mL 11.2481 mL 22.4962 mL 56.2404 mL
    5 mM 0.4499 mL 2.2496 mL 4.4992 mL 11.2481 mL
    10 mM 0.2250 mL 1.1248 mL 2.2496 mL 5.6240 mL
    15 mM 0.1500 mL 0.7499 mL 1.4997 mL 3.7494 mL
    20 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8120 mL
    25 mM 0.0900 mL 0.4499 mL 0.8998 mL 2.2496 mL
    30 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8747 mL
    40 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
    50 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
    60 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
    80 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
    100 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
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    Canagliflozin Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

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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:

    Canagliflozin842133-18-0JNJ 28431754JNJ28431754JNJ-28431754SGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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