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5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽

5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽

中文名稱5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽
中文同義詞5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽;PPARΓ激動(dòng)劑(INOLITAZONE DIHYDROCHLORIDE);化合物 T15580;化合物 INOLITAZONE DIHYDROCHLORIDE
英文名稱CS 7017
英文同義詞CS 7017;Inolitazone (dihydrochloride);5-[[4-[[6-(4-Amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-thiazolidinedione dihydrochloride;Inolitazone (CS-7017) dihydrochloride;RS5444 dihydrochloride;Inolitazone (CS-7017) 2HCl;5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methylbenzimidazol-2-yl]methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione;EFATUTAZONE; CS-7017; RS5444; CS 7017; RS 5444
CAS號(hào)223132-38-5
分子式C27H28Cl2N4O4S
分子量575.50662
EINECS號(hào)
相關(guān)類別細(xì)胞生物學(xué)試劑
Mol文件223132-38-5.mol
結(jié)構(gòu)式5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽 結(jié)構(gòu)式

5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽 性質(zhì)

儲(chǔ)存條件Store at -20°C
溶解度DMSO:25 mg/mL(43.44 mM;需要超聲波)H2O:< 0.1 mg/mL(不溶)
形態(tài)粉末
顏色淺紫色至紫色

5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽 用途與合成方法

Inolitazone dihydrochloride (Efatutazone dihydrochloride) 是一種高親和力的 PPARγ 激動(dòng)劑,活性依賴于 PPARγ,抑制生長(zhǎng),IC50 為 0.8 nM。

PPARγ

Inolitazone dihydrochloride (Efatutazone dihydrochloride) upregulates the cell cycle kinase inhibitor, p21 WAF1/CIP1 . Silencing p21 WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM 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 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.
DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism.

Inolitazone dihydrochloride (Efatutazone dihydrochloride) 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.

安全信息

MSDS信息

更新日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2026/06/05HY-14792BR5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽
Inolitazone dihydrochloride (Standard)
223132-38-51 mg1280元
2026/06/05HY-14792BR5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽
Inolitazone dihydrochloride (Standard)
223132-38-55 mg3200元

5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽 上下游產(chǎn)品信息

"5-[[4-[[6-(4-氨基-3,5-二甲基苯氧基)-1-甲基-1H-苯并咪唑-2-基]甲氧基]苯基]甲基]-2,4-噻唑烷二酮二鹽酸鹽"相關(guān)產(chǎn)品信息
對(duì)二甲苯 丁基氨基甲酸碘代丙炔酯 氯化芐 2,6-二甲基苯胺 N,N-二甲基苯胺
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