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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10 mM * 1 mL in DMSO USD 61 In-stock
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ready for reconstitution
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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 27 publication(s) in Google Scholar

Other Forms of Canagliflozin:

Top Publications Citing Use of Products

    Canagliflozin purchased from MCE. 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 MCE. 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 MCE. 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].

    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].

    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

    Appearance

    Solid

    Formula

    C24H25FO5S

    CAS No.
    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)

    *"≥" 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.68 mM); Clear solution

    • 6.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (1.12 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.80%

    References
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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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    This equation is commonly abbreviated as: C1V1 = C2V2

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    Product Name:
    Canagliflozin
    Cat. No.:
    HY-10451
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