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 분자식: C₂₂H₂₄O₄S 분자량: 384.49 EC 번호: 815-538-9

등급 & 순도 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

개요

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%

사양

동의어

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

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

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

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.

등급

Moligand™

작업 유형

AGONIST

작동 메커니즘

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

제품 특성

ALogP

5.477

hba_count

3

회전 가능한 결합

7

이름과 식별자

이성체 SMILES

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

분자량

384.49

Reaxy-Rn

24554260

Reaxys-RN_link_address

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

관련 대상(인간)

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)

화학 및 물리적 특성

• 용해성: Solubility (25°C) In vitro DMSO: 29 mg/mL (195.68 mM)
• DMSO(mg/mL) 최대 용해도: 76
• DMSO(mM) 최대 용해도: 197.6644386
• 물(mg/mL) 최대 용해도: ＜1