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Inolitazone

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Catalog No. T15581Cas No. 223132-37-4
Alias RS5444, Efatutazone, CS-7017

Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.

Inolitazone

Inolitazone

😃Good
Purity: 99.53%
Catalog No. T15581Alias RS5444, Efatutazone, CS-7017Cas No. 223132-37-4
Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$67In StockIn Stock
5 mg$160In StockIn Stock
10 mg$256In StockIn Stock
25 mg$415In StockIn Stock
50 mg$592In StockIn Stock
100 mg$793In StockIn Stock
500 mgPreferential-In Stock
1 mL x 10 mM (in DMSO)$198In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.53%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.
In vitro
Inolitazone (10 nM) inhibits the growth of DRO cells through a PPARγ-dependent mechanism[1]. Inolitazone upregulates the cell cycle kinase inhibitor, p21WAF1/CIP1. Inolitazone (10 nM) activates PPARγ:RXRα-dependent transcription utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Inolitazone (10 nM) 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[2].
In vivo
In athymic nude mice prior to DRO tumor cell implantation, Inolitazone inhibits tumor growth in a dose responsive fashion. 0.025% Inolitazone inhibits growth on day 32 by 94.4%. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors on day 35. Inolitazone plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth[1].
SynonymsRS5444, Efatutazone, CS-7017
Chemical Properties
Molecular Weight502.58
FormulaC27H26N4O4S
Cas No.223132-37-4
SmilesCN1C=2C(N=C1COC3=CC=C(CC4C(=O)NC(=O)S4)C=C3)=CC=C(OC5=CC(C)=C(N)C(C)=C5)C2
Relative Density.1.39 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (109.44 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9897 mL9.9487 mL19.8973 mL99.4866 mL
5 mM0.3979 mL1.9897 mL3.9795 mL19.8973 mL
10 mM0.1990 mL0.9949 mL1.9897 mL9.9487 mL
20 mM0.0995 mL0.4974 mL0.9949 mL4.9743 mL
50 mM0.0398 mL0.1990 mL0.3979 mL1.9897 mL
100 mM0.0199 mL0.0995 mL0.1990 mL0.9949 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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