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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
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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)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ApexBio Technology
Product number
A3498
Product name
Inolitazone
Packaging
2mg
Price
$350
Updated
2021/12/16
ApexBio Technology
Product number
A3498
Product name
Inolitazone
Packaging
5mg
Price
$524
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
INB0004454
Product name
INOLITAZONE
Purity
95.00%
Packaging
5MG
Price
$672.1
Updated
2021/12/16
Crysdot
Product number
CD31002616
Product name
Inolitazone
Purity
98+%
Packaging
5mg
Price
$233
Updated
2021/12/16
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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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inolitazone Suppliers

China 44 United States 7 Global 51
MedChemexpress LLC
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021-58955995
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609-228-5909
Email
sales@medchemexpress.cn
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United States
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Musechem
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+1-800-259-7612
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+1-800-259-7612
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info@musechem.com
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United States
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TargetMol Chemicals Inc.
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+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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United States
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32165
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Cckinase, Inc.
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+1 (732)236-3202
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sales@cckinase.com
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United States
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2738
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58
Aladdin Scientific
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+1-+1(833)-552-7181
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sales@aladdinsci.com
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United States
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52925
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58
ApexBio Technology
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sales@apexbt.com
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United States
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6251
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MedChemExpress
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sales@medchemexpress.com
Country
United States
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6398
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58

223132-37-4, inolitazoneRelated Search:

Iodopropynyl butylcarbamate Benzyl chloride 2,6-Dimethylaniline N,N-Dimethylaniline P-XYLENE

  • CS-1166
  • Inolitazone Efatutazone
  • inolitazone
  • 5-[[4-[[6-(4-Amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-thiazolidinedione
  • Efatutazone
  • RS5444
  • Inolitazone (CS-7017)
  • 2,4-Thiazolidinedione, 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-
  • CS 7017,Inolitazone,PPAR,Peroxisome proliferator-activated receptors,CS7017,RS 5444,Inhibitor,RS-5444,inhibit
  • 223132-37-4