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

Canagliflozin hemihydrate (Synonyms: JNJ 24831754ZAE (hemihydrate); JNJ 28431754 (hemihydrate); JNJ 28431754AAA (hemihydrate); TA 7284 (hemihydrate))

Cat. No.: HY-I0383 Purity: 99.95%
Handling Instructions

Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-7284 hemihydrate) 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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Canagliflozin hemihydrate Chemical Structure

Canagliflozin hemihydrate Chemical Structure

CAS No. : 928672-86-0

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Canagliflozin hemihydrate:

Top Publications Citing Use of Products

    Canagliflozin hemihydrate purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59.

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

    Canagliflozin hemihydrate purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59.

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

    Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-7284 hemihydrate) 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

    IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells)[1]

    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].

    In Vivo

    Canagliflozin (30 mg/kg treatment for 4 weeks) reduced 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].

    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

    453.52

    Formula

    C₂₄H₂₆FO₅.₅S

    CAS No.

    928672-86-0

    SMILES

    CC1=CC=C([[email protected]]2[[email protected]](O)[[email protected]@H](O)[[email protected]](O)[[email protected]@H](CO)O2)C=C1CC3=CC=C(C4=CC=C(F)C=C4)S3.[0.5H2O]

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (220.50 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2050 mL 11.0249 mL 22.0497 mL
    5 mM 0.4410 mL 2.2050 mL 4.4099 mL
    10 mM 0.2205 mL 1.1025 mL 2.2050 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.95%

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    Product Name:
    Canagliflozin hemihydrate
    Cat. No.:
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