Elafibranor | CAS:923978-27-2

• 価格
• 構造式
• 製品情報
• 製品詳細
• 文献

価格

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構造式

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製品情報

Elafibranor is an agonist of the peroxisome proliferator-activated receptors (PPAR) α and δ. It increases HDL secretion and expression of the lipid-related genes ABCA1, PLIN-2, and ABHD5 in Caco-2/TC7 cells in a PPARα-dependent manner. Elafibranor (10 mg/kg) decreases levels of plasma triglycerides and total cholesterol while increasing plasma HDL and expression of Acox1, a PPARα target gene, in the liver of ApoE2-KI wild-type, but not PPARα knockout, mice fed a Western diet. However, PPARα knockout mice exhibit a decrease in plasma total and non-HDL cholesterol levels, indicating PPARδ has a role in these functions. Elafibranor (30 mg/kg) reduces diet-induced macro- and micro-steatosis in a PPARα-deficient mouse model of non-alcoholic steatohepatitis. It also reduces cholesterol and triglyceride accumulation as well as macrovesicular steatosis in the liver of insulin-resistant db/db mice fed the methionine-choline deficient (MCD) diet. Formulations containing elafibranor are under clinical investigation for the treatment of non-alcoholic steatohepatitis.

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製品詳細

name	Elafibranor
Formal Name	2-[2,6-dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl-propanoic acid
CAS Number	923978-27-2
Synonyms	GFT505
Molecular Formula	C22H24O4S
Formula Weight	384.5
Purity	≥98%
Formulation	A solid
SMILES	CSC1=CC=C(C(/C=C/C2=CC(C)=C(OC(C)(C)C(O)=O)C(C)=C2)=O)C=C1
InChI Code	InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+
InChI Key	AFLFKFHDSCQHOL-IZZDOVSWSA-N
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
Stability	≥ 2 years

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文献

1. Colin, S., Briand, O., Touche, V., et al. Activation of intestinal peroxisome proliferator-activated receptor-α increases high-density lipoprotein production. Eur. Heart J. 34(32), 2566-2574 (2013).

2. Staels, B., Rubenstrunk, A., Noel, B., et al. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis. Hepatology 58(6), 1941-1952 (2013).

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