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トログリタゾン

トログリタゾン 化学構造式
97322-87-7
CAS番号.
97322-87-7
化学名:
トログリタゾン
别名:
トログリタゾン;トログリタゾン (JAN)
英語化学名:
Troglitazone
英語别名:
ci991;CS-045;Noscal;rezulin;Depotox;gr92132x;AKOS 91980;ROMGLIZONE;RESULIN(TM);TROGLITAZONE
CBNumber:
CB0486895
化学式:
C24H27NO5S
分子量:
441.54
MOL File:
97322-87-7.mol

トログリタゾン 物理性質

融点 :
184-186°C
貯蔵温度 :
Store at -20°C
溶解性:
DMSO: 20 mg/mL
外見 :
solid
色:
white to yellow
InChIKey:
GXPHKUHSUJUWKP-UHFFFAOYSA-N
CAS データベース:
97322-87-7(CAS DataBase Reference)

安全性情報

Sフレーズ  22-24/25
WGK Germany  2
RTECS 番号 XJ5813130
HSコード  29145090

トログリタゾン 価格 もっと(19)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01CAY71750
Troglitazone
97322-87-7 5mg ¥10800 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01BVI1696-5
Troglitazone
97322-87-7 5mg ¥27300 2018-12-26 購入
Sigma-Aldrich Japan T2573 トログリタゾン ≥98% (HPLC)
Troglitazone ≥98% (HPLC)
5mg ¥36000 2018-12-25 購入
富士フイルム和光純薬株式会社(wako) W01W0120-1948 トログリタゾン 97.0+% (HPLC)
Troglitazone 97.0+% (HPLC)
97322-87-7 50mg ¥51000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01W0120-1760 トログリタゾン 98.0+%(HPLC)
Troglitazone 98.0+%(HPLC)
97322-87-7 50mg ¥55000 2018-12-26 購入

トログリタゾン MSDS


Troglitazone

トログリタゾン 化学特性,用途語,生産方法

外観

白色〜褐色, 結晶〜結晶性粉末

溶解性

メタノール-ジメチルスルホキシド溶状:試験適合

効能

糖尿病治療薬, ペルオキシソーム増殖因子活性化受容体(PPAR)γ作動薬

説明

Rezulin was launched in Japan, the UK (subseqently withdrawn) and the US for treatment of type Ⅱ diabetes. Two approaches, four steps and six steps, converge on 6-acetoxy-2-(4-aminophenoxymethyl)-2,5,7,8-tetramethylchroman which can be elaborated in two steps to Rezulin. It is the first of a new class of thiazolidenediones for NIDDM that reduces glucose concentrations without effecting insulin secretion. It binds to peroxisome proliferator-activated receptor gamma (PPARγ) thus activating this nuclear receptor which then influences carbohydrate metabolism. This is accomplished by increasing insulin sensitivity by upregulating glucose transporter (Glut1 and/or Glut4) expression without affecting the number or affinity of insulin receptors. There is also an increase in hepatic glycogen synthase activity which enhances glucose utilization and a reduction in hepatic gluconeogenesis by inhibiting fructose-1 ,&bisphosphatase. Pancreatic islet cell destruction is prevented. It reduces serum triglycerides because PPARγ causes fibroblasts to differentiate into adipocytes and does not activate RARα. It has a half-life of 9 h and is metabolized into three compounds having no activity.

化学的特性

Crystalline Solid

Originator

Sankyo (Japan)

使用

Troglitazone is an an oral hypoglycemic agent which improves insulin sensitivity and decreases hepatic glucose production. Antidiabetic.

使用

antidiabetic;peroxisome proliferator-activated receptors activator

使用

Troglitazone is a TZD which was approved for the treatment of insulin resistance and hyperglycemia in Type II diabetes, under the trade name Resulin?, but was withdrawn from the market due to hepatotoxicity. Troglitazone is a potent and selective PPARγ agonist. The EC50 values for transactivation of human and mouse PPARγ in a cell-based assay are 0.55 and 0.78 μM, respectively. In the same assay system, no activation of PPARα and PPARδ was observed at concentrations up to 10 μM. Troglitazone binds to the PPARγ ligand-binding domain (LBD) but fails to induce interaction of the PPARγ LBD with the transcriptional coactivators SRC-1, TIF2, AIB1, p300, or TRAP220. Troglitazone also induces cell cycle arrest and apoptosis in several cancer cell lines with an EC50 of 10 μM.

brand name

Prelay (Sankyo); Rezulin (Pfizer);Ronglitazone.

生物活性

Selective PPAR γ receptor agonist (EC 50 values are 780 and 555 nM at murine and human PPAR γ receptors respectively). Displays no activity at PPAR α or PPAR δ receptors. Antidiabetic agent; exerts potent glucose-lowering effects in insulin-resistant diabetic mice. Displays anti-invasive effect on human breast cancer cells; reduces migration, adhesion and spreading on fibronectin-coated plates. Also inhibits lamellipodia formation and actin polymerization.

トログリタゾン 上流と下流の製品情報

原材料

準備製品


トログリタゾン 生産企業

Global( 104)Suppliers
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97322-87-7(トログリタゾン)キーワード:


  • 97322-87-7
  • 5-(4-(6-hydroxy-2,5,7,8-tetramethylchroman-2-ylmethoxy)benzyl)thiazolidine-2
  • ci991
  • enzopyran-2-yl)methoxy)phenyl)methyl)-
  • gr92132x
  • rezulin
  • CS-045
  • Troglitazone - CAS 97322-87-7 - Calbiochem
  • 2,4-thiazolidinedione,5-((4-((3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2h-1-b
  • CI-991,NOSCAL
  • AKOS 91980
  • (+/-)-5-[4-[(6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMAN-2-YL)METHOXY]BENZYL]-2,4-THIAZOLIDINEDIONE
  • 5-[[4-[(3,4-DIHYDRO-6-HYDROXY-2,5,7,8-TETRAMETHYL-2H-1-BENZOPYRAN-2-YL)METHOXY]-PHENYL]METHYL]-2,4-THIAZOLIDINEDIONE
  • 5-[[4-((3,4-DIHYDRO-6-HYDROXY-2,5,7,8-TETRAMETHYL-2H-1-BENZOPYRAN-2-YL)METHOXY)PHENYL]METHYL]-2,4-TH
  • 5-[[4-[(3,4-DIHYDRO-6-HYDROXY-2,5,7,8-TETRAMETHYL-2H-1-BENZOPYRAN-2-YL)METHOXY]PHENYL]METHYL]-2,4-THIOAZOLIDINEDIONE
  • TroglitazoneMesylate
  • 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]-phenyl]methyl]-2,4-thiazolidinedione, Romglizone, CS-045, CI-991,Noscal,
  • Troglitazone for research
  • CS-045, (±)-5-[4-[(6-Hydroxy-2,5,7,8-tetramethylchroman-2-yl)methoxy]benzyl]-2,4-thiazolidinedione
  • 5-(4-[(6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)methoxy]benzyl)thiazolidine-2,4-dione
  • 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-y1)methoxy]phenyl]methyl]-2.4-thiazolidinedione
  • 2,4-Thiazolidinedione, 5-((4-((3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl) methoxy)phenyl)methyl)
  • 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-2,4-thiazolidinedione
  • Depotox
  • Noscal
  • Troglitazone(Rezulin)
  • Troglitazone, >=98%
  • Troglitazone(CS-045)
  • RESULIN(TM)
  • ROMGLIZONE
  • TROGLITAZONE
  • トログリタゾン
  • トログリタゾン (JAN)
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