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

Canagliflozin  (Synonyms: JNJ 28431754)

Cat. No.: HY-10451 Purity: 99.80%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Canagliflozin Chemical Structure

Canagliflozin Chemical Structure

CAS No. : 842133-18-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 61 In-stock
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10 mg USD 77 In-stock
50 mg USD 121 In-stock
100 mg USD 154 In-stock
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Customer Review

Based on 31 publication(s) in Google Scholar

Other Forms of Canagliflozin:

Top Publications Citing Use of Products

    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).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    In Vitro

    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.

    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    444.52

    Formula

    C24H25FO5S

    CAS No.
    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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
    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
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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

    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.
    Purity & Documentation

    Purity: 99.80%

    References

    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

    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.

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    Product Name:
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    Cat. No.:
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