inolitazone

Product Name: inolitazone
CAS No.: 223132-37-4
Chemical Name: inolitazone
Synonyms: RS5444;CS-1166;Efatutazone;inolitazone;Inolitazone (CS-7017);Inolitazone Efatutazone;Inolitazone, 10 mM in DMSO;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)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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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

Uses

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

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

IC 50

PPARγ

References

[1] Copland JA, et al. Novel high-affinity PPARgamma agonist alone and in combination with paclitaxel inhibits human anaplastic thyroid carcinoma tumor growth via p21WAF1/CIP1. Oncogene. 2006 Apr 13;25(16):2304-17. DOI:10.1038/sj.onc.1209267
[2] Marlow LA, et al. Reactivation of suppressed RhoB is a critical step for the inhibition of anaplastic thyroid cancer growth. Cancer Res. 2009 Feb 15;69(4):1536-44. DOI:10.1158/0008-5472.CAN-08-3718

inolitazone Preparation Products And Raw materials

Raw materials

Preparation Products

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inolitazone Suppliers

China 51 United States 7 Global 58

Shanghai Boyle Chemical Co., Ltd.

Tel
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Country: China
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NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
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MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
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CEG Chemical Science&Technology Co., Ltd.

Tel: Mobile:13665161512
Fax: +86-510-68873513
Country: China
ProdList: 1785
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ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
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Country: China
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LETOPHARM LIMITED

Tel: +86-21-5821 5861
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Email: sales@letopharm.com
Country: China
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Codow Chemical Co.,Ltd.

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Email: amy@howeipharm.com
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Chengdu Huachun Technology Co., Ltd

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Shanghai Biopharmaleader Co., Ltd.

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Musechem

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223132-37-4, inolitazoneRelated Search:

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

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

Inolitazone, 10 mM in DMSO

223132-37-4