inolitazone
- Product Name
- inolitazone
- CAS No.
- 223132-37-4
- Chemical Name
- inolitazone
- Synonyms
- RS5444;CS-1166;Efatutazone;inolitazone;Inolitazone (CS-7017);Inolitazone Efatutazone;CS 7017,Inolitazone,PPAR,Peroxisome proliferator-activated receptors,CS7017,RS 5444,Inhibitor,RS-5444,inhibit;5-[[4-[[6-(4-Amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-thiazolidinedione;2,4-Thiazolidinedione, 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-
- CBNumber
- CB51518514
- Molecular Formula
- C27H26N4O4S
- Formula Weight
- 502.58
- MOL File
- 223132-37-4.mol
inolitazone Property
- Boiling point:
- 765.7±60.0 °C(Predicted)
- Density
- 1.39
- storage temp.
- Store at -20°C
- solubility
- DMSO
- form
- Powder
- pka
- 6.34±0.50(Predicted)
N-Bromosuccinimide Price
- Product number
- A3498
- Product name
- Inolitazone
- Packaging
- 2mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- A3498
- Product name
- Inolitazone
- Packaging
- 5mg
- Price
- $524
- Updated
- 2021/12/16
- Product number
- INB0004454
- Product name
- INOLITAZONE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $672.1
- Updated
- 2021/12/16
- Product number
- CD31002616
- Product name
- Inolitazone
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $233
- Updated
- 2021/12/16
inolitazone Chemical Properties,Usage,Production
Biological Activity
Inolitazone (RS5444; CS-7017) is a novel high-affinity agonist of PPARγ with one-fifth EC50 of rosiglitazone, and has no inhibitory effect on RIE cells that do not express PPARγ.
in vitro
Inolitazone (RS5444) upregulates the cell cycle kinase inhibitor, p21 WAF1/CIP1 . Silencing p21 WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM The 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 EC 50 occurs. The EC 50 s are 1 nM (Inolitazone), 65 nM (Rosiglitazone) and 631 nM (Troglitazone). Similarly, the calculated inhibitory concentration at IC 50 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 tran sient 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. DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism.
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.
target
| PPARγ
|
inolitazone Preparation Products And Raw materials
Raw materials
Preparation Products
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