1. Cell Cycle/DNA Damage
  2. PPAR
  3. Inolitazone dihydrochloride

Inolitazone dihydrochloride (Synonyms: Efatutazone (dihydrochloride); CS-7017 (dihydrochloride); RS5444 (dihydrochloride))

Cat. No.: HY-14792B Purity: 99.21%
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Inolitazone dihydrochloride is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.

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

Inolitazone dihydrochloride Chemical Structure

Inolitazone dihydrochloride Chemical Structure

CAS No. : 223132-38-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 544 In-stock
Estimated Time of Arrival: December 31
5 mg USD 430 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Inolitazone dihydrochloride:

Top Publications Citing Use of Products

    Inolitazone dihydrochloride purchased from MCE. Usage Cited in: Cancer Med. 2018 May;7(5):1955-1966.

    Protein expression in cells incubated with 40 μM Efatutazone for 12, 24, and 48 h.

    Inolitazone dihydrochloride purchased from MCE. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256.

    Western blot analysis for p21, p-p21, Cyclin D1. Bcl-2, Caspase 3, Cleaved Caspase 3, Caspase 9, Cleaved Caspase 9 and Bax in HCC827-GR and PC-9-GR cells treated with control, Efatutazone alone, Gefitinib alone, or Efatutazone combined with gefitinib for 48 h.

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    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    Inolitazone dihydrochloride is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.

    IC50 & Target[1]

    PPARγ

     

    In Vitro

    Inolitazone (RS5444) dihydrochloride upregulates the cell cycle kinase inhibitor, p21WAF1/CIP1. Silencing p21WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM dose of Inolitazone activates PPARγ:RXRα-dependent transcription as demonstrated in a transient transfection assay utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). DRO cells are treated in culture with Inolitazone, Rosiglitazone, or Troglitazone at the indicated concentrations. DRO cells are transiently transfected with PPRE3-tk-luc to examine effective concentrations at which EC50 occurs. The EC50s are 1 nM (Inolitazone), 65 nM (Rosiglitazone) and 631 nM (Troglitazone). Similarly, the calculated inhibitory concentration at IC50 is 0.8 nM for Inolitazone, 75 nM for Rosiglitazone, and 1412 nM for Troglitazone. Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Exposure of 10 nM Inolitazone following transient transfection with the appropriate PPAR isoform (γ, α, or δ) and PPAR response element linked to a luciferase reporter in RIE rat small intestinal cell line, which does not express PPARs, yields increased luciferase activity only in the presence of PPARγ and PPRE3-tk-luc[1]. DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism[2].

    In Vivo

    Inolitazone (RS5444) plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth. When Inolitazone is administered in the diet to athymic nude mice prior to DRO tumor cell implantation, tumor growth is inhibited in a dose responsive fashion. At the highest dose, 0.025% Inolitazone inhibits growth on day 32 by 94.4% as compared to that of control. In this treatment group, five of 10 animals do not develop demonstrable tumors. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% compared to that of control on day 32 while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Tumors is nest allowed to establish in the mouse and began 0.025% Inolitazone treatment of mice 1 week after DRO or ARO tumor cell implantation. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors as compared to that of their respective controls on day 35[1].

    Clinical Trial
    Molecular Weight

    575.51

    Formula

    C₂₇H₂₈Cl₂N₄O₄S

    CAS No.

    223132-38-5

    SMILES

    O=C(N1)SC(CC2=CC=C(OCC3=NC4=CC=C(OC5=CC(C)=C(N)C(C)=C5)C=C4N3C)C=C2)C1=O.Cl.Cl

    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 : 25 mg/mL (43.44 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7376 mL 8.6879 mL 17.3759 mL
    5 mM 0.3475 mL 1.7376 mL 3.4752 mL
    10 mM 0.1738 mL 0.8688 mL 1.7376 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 (4.34 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    DRO90-1 (DRO) and ARO81 (ARO) cells are plated in 12-well culture plates in triplicate for each condition at an initial concentration of 2×104 cells/well. After overnight incubation, cells are treated with either Inolitazone, Rosiglitazone, Troglitazone, GW9662, or Paclitaxel diluted in DMSO at concentrations indicated in figure legends. All cells receive identical volumes of DMSO and are exposed to each drug for 6 days with medium and drug changed every 48 h. After 6 days, cells are washed with PBS, trypsinized and counted by Beckman Coulter Counter[1].

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

    Animal Administration
    [1]

    Mice[1]
    Suspensions of 1×106/0.1 mL DRO or ARO cells in RPMI medium are injected subcutaneously in one flank of 3-4 week athymic female nude mice. Mice are changed to specialized diets either 1 week prior or 1 week after tumor implantation and randomly assigned to experimental or control groups with 10 mice per group. Diets consisted either placebo, 0.00025%, 0.0025%, or 0.025% Inolitazone formulated into the diet. Mice weighed between 20-25 g and consume on average 4 g of food per day. For combinatorial studies either placebo, 10 mg/kg or 15 mg/kg paclitaxel is injected i.p. twice weekly. Tumors are measured every 3-4 days for 35 days with calipers and tumor volumes are calculated by the formula: 0.5236(a×b×c), where a is the shortest diameter, b is the diameter perpendicular to a and c is the diameter height.

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

    References
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    Keywords:

    InolitazoneEfatutazoneCS-7017RS5444CS7017CS 7017RS 5444RS-5444PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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    Product name:
    Inolitazone dihydrochloride
    Cat. No.:
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