DC Chemicals Limited
China
Product Name: Elafibranor(GFT505)
Price: $550.0/100mg $750.0/250mg $1350.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Elafibranor
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

923978-27-2

923978-27-2 structure

923978-27-2 structure

Name: Elafibranor
Chemical Name: (E)-Elafibranor
CAS Number: 923978-27-2
Molecular Formula: C₂₂H₂₄O₄S
Molecular Weight: 384.489
Catalog: Organic raw materials Carboxylic compounds and derivatives Halogenation, sulfonation, nitration or nitration of carboxylic anhydrides
Create Date: 2018-04-25 05:52:27
Modify Date: 2024-01-06 19:13:28
Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.

Name	(E)-Elafibranor
Synonyms	UNII-2J3H5C81A5 2-(2,6-Dimethyl-4-{(1E)-3-[4-(methylsulfanyl)phenyl]-3-oxo-1-propen-1-yl}phenoxy)-2-methylpropanoic acid Propanoic acid, 2-[2,6-dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl- GFT505 Elafibranor 2-[2,6-Dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methylpropanoic acid

Description	Elafibranor is a PPARα/δ agonist with EC50s of 45 and 175 nM, respectively.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR Research Areas >> Metabolic Disease
Target	PPAR-α:45 nM (EC50) PPAR-δ:175 nM (EC50)
In Vitro	GFT505 is being developed as a dual PPAR-α/PPAR-δ agonist for the treatment of T2DM and non-alcoholic fatty liver disease. GFT505 has an active metabolite, GFT1007, and both have potent agonist activity for PPAR-α and to a lesser extent for PPAR-δ[1].
In Vivo	GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study[1]. Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation[2]. GFT505 treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys[3].
References	[1]. Liu ZM, et al. Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.Expert Opin Investig Drugs. 2015 May;24(5):611-21. [2]. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016 May;150(5):1147-1159. [3]. Hanf R, et al. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.Diab Vasc Dis Res. 2014 No

Density	1.2±0.1 g/cm3
Boiling Point	569.0±50.0 °C at 760 mmHg
Molecular Formula	C₂₂H₂₄O₄S
Molecular Weight	384.489
Flash Point	297.9±30.1 °C
Exact Mass	384.139526
LogP	5.63
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.606
Storage condition	2-8°C