Name: 罗格列酮, FFA1 受体激动剂；过氧化物酶体增殖激活受体-γ 激动剂；TRPC5 激活剂；TRPM3 通道阻断剂
SKU: R408369
Availability: InStock

罗格列酮, FFA1 受体激动剂；过氧化物酶体增殖激活受体-γ 激动剂；TRPC5 激活剂；TRPM3 通道阻断剂

CAS: 122320-73-4 货号: R408369 分子式: C₁₈H₁₉N₃O₃S 分子量: 357.43 EC号: 924-121-1 PubChem CID: 77999

概述规格名称和识别符技术文档高级数据关联靶点（人）质检证书（CoA,COO,BSE/TSE 和分析图谱) 化学和物理性质安全和危险性（GHS）此产品的引用文献技术文档和文章溶液计算器

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为什么选择此级别

Moligand™ 级，适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 39 篇同行评审文献引用。

概述

A potent and selective PPARγ agonist.

Information

Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of P
In vitro

Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. Rosiglitazone activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase. Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro. Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.

In vivo

Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. Rosiglitazone also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. Rosiglitazone decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased. Rosiglitazone upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure.
Cell Data

cell lines：RAW 264.7 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

规格

英文别名

5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-tiazolidinedione

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Rosiglitazone (BRL 49653)

生化机理

罗格列酮（BRL 49653）是一种强效降血糖药和强效噻唑烷二酮胰岛素增敏剂，对大鼠、3T3-L1 和人类脂肪细胞的 IC50 分别为 12、4 和 9 nM。罗格列酮是 PPAR-gamma 的纯配体，没有与 PPAR-α 结合的作用。罗格列酮能调节 TRP 通道并诱导自噬。罗格列酮能防止铁氧化。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

激动剂

作用机制

FFA1 受体激动剂；过氧化物酶体增殖激活受体-γ 激动剂；TRPC5 激活剂；TRPM3 通道阻断剂

名称和识别符

EC号

924-121-1

分子类型