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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $67 | In Stock | In Stock | |
| 5 mg | $160 | In Stock | In Stock | |
| 10 mg | $256 | In Stock | In Stock | |
| 25 mg | $415 | In Stock | In Stock | |
| 50 mg | $592 | In Stock | In Stock | |
| 100 mg | $793 | In Stock | In Stock | |
| 500 mg | Preferential | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $198 | In Stock | In Stock |
| 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]. |
| Synonyms | RS5444, Efatutazone, CS-7017 |
| Molecular Weight | 502.58 |
| Formula | C27H26N4O4S |
| Cas No. | 223132-37-4 |
| Smiles | CN1C=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 | Powder: -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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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