Elafibranor - Moligand™, 10mM in DMSO , Agonist of Peroxisome proliferator-activated receptor-α;Agonist of Peroxisome proliferator-activated receptor-γ, CAS No.923978-27-2, Agonist of Peroxisome proliferator-activated receptor-α;Agonist of Peroxisome proliferator-activated receptor-γ

CAS: 923978-27-2 Cat. No.: E408744 分子式: C₂₂H₂₄O₄S 分子量: 384.49 EC番号: 815-538-9

グレード＆純度 Moligand™, 10mM in DMSO

Synonyms

GFT505 | Propanoic acid, 2-​[2,​6-​dimethyl-​4-​[(1E)​-​3-​[4-​(methylthio)​phenyl]​-​3-​oxo-​1-​propen-​1-​yl]​phenoxy]​-​2-​methyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Elafibranor (GFT505) is an agonist of theperoxisome proliferator-activated receptor-α(PPAR-alpha)andperoxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation.
In vitro

GFT505 is a novel PPAR modulator that shows a preferential activity on PPAR-α and concomitant activity on PPAR-δ.

In vivo

Elafibranor (GFT505) is a dual PPARα/δ agonist that has demonstrated efficacy in disease models of nonalcoholic fatty liver disease (NAFLD)/NASH and liver fibrosis. In the rat, GFT505 concentrated in the liver with limited extrahepatic exposure and underwent extensive enterohepatic cycling. Elafibranor confers liver protection by acting on several pathways involved in NASH pathogenesis, reducing steatosis, inflammation, and fibrosis. GFT505 improved liver dysfunction markers, decreased hepatic lipid accumulation, and inhibited proinflammatory (interleukin-1 beta, tumor necrosis factor alpha, and F4/80) and profibrotic (transforming growth factor beta, tissue inhibitor of metalloproteinase 2, collagen type I, alpha 1, and collagen type I, alpha 2) gene expression.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

仕様

同義語

GFT505 | Propanoic acid, 2-​[2,​6-​dimethyl-​4-​[(1E)​-​3-​[4-​(methylthio)​phenyl]​-​3-​oxo-​1-​propen-​1-​yl]​phenoxy]​-​2-​methyl-

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α(PPAR-alpha) and peroxisome proliferator-activated receptor-δ(PPAR-δ). It improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammatio

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

AGONIST

作用メカニズム

Agonist of Peroxisome proliferator-activated receptor-α;Agonist of Peroxisome proliferator-activated receptor-γ

製品の性質

ALogP

5.477

hba_count

3

回転可能な結合

7

名前と識別子

異性体SMILES

CC1=CC(=CC(=C1OC(C)(C)C(=O)O)C)/C=C/C(=O)C2=CC=C(C=C2)SC

分子量

384.49

Reaxy-Rn

24554260

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24554260&ln=

関連ターゲット（人間）

PPARA Tclin Peroxisome proliferator-activated receptor alpha (0 Activities)

Discover Target: PPARA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARD Tchem Peroxisome proliferator-activated receptor delta (0 Activities)

Discover Target: PPARD

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 29 mg/mL (195.68 mM)
• DMSO（mg / mL） 最大溶解度: 76
• DMSO（mM） 最大溶解度: 197.6644386
• 水（mg / mL） 最大溶解度: ＜1