923978-27-2 Usage
Description
Elafibranor (GFT505) is a dual peroxisome proliferator-activated receptor (PPAR) α and δ agonist that modulates lipid metabolism and has potential therapeutic effects in the treatment of non-alcoholic steatohepatitis (NASH).
Used in Pharmaceutical Industry:
Elafibranor (GFT505) is used as a therapeutic agent for the treatment of non-alcoholic steatohepatitis (NASH) due to its ability to modulate lipid metabolism and reduce liver steatosis.
Used in Clinical Research:
Elafibranor (GFT505) is used as a subject of clinical investigation for its potential therapeutic effects in the treatment of non-alcoholic steatohepatitis (NASH) and related liver diseases.
Biological Functions
Elafibranor (GFT505) is an agonist of peroxisome proliferator-activated receptor (PPAR) alpha and delta. EC50 values were 45 and 175 nM, respectively. GFT505 is being developed as a dual PPAR-α/PPAR-δ receptor agonist for the treatment of type 2 diabetes and nonalcoholic fatty liver disease. GFT1007 and GFT505 have an active metabolite, both with potent stimulant activity PPAR-α and to a lesser extent PPAR-δ.
Biological Activity
Elafibranor (GFT505) is an agonist of PPAR-alpha and PPAR-delta, improves insulin sensitivity, benefits glucose homeostasis, lipid metabolism and reduces inflammation.
References
1) Cariou?et al.?(2011)?Effects of the New Dual PPARα/δ Agonist GFT505 on Lipid and Glucose Homeostasis in Abdominally Obese Patients With Combined Dyslipidemia or Impaired Glucose Metabolism; Diabetes Care?34?2008
2) Cariou?et al.?(2013)?Dual peroxisome proliferator receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects; Diabetes Care?36?2923
3) Hanf?et al.?(2014)?The dual peroxisome proliferator-activated 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.?11?440
4) Staels?et al.?(2013)?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?1941
5) Ratziu?et al.?(2016)?Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.; Gastroenterology.?39?2951
6) Boeckmans?et al. (2019)?Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH.; Pharmacol. Res.?114?377
Check Digit Verification of cas no
The CAS Registry Mumber 923978-27-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,3,9,7 and 8 respectively; the second part has 2 digits, 2 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 923978-27:
(8*9)+(7*2)+(6*3)+(5*9)+(4*7)+(3*8)+(2*2)+(1*7)=212
212 % 10 = 2
So 923978-27-2 is a valid CAS Registry Number.
923978-27-2Relevant articles and documents
POLYMORPHS OF ELAFIBRANOR
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Page/Page column 23-24, (2021/08/20)
The present invention relates to novel crystalline forms of elafibranor.
PROCESS FOR PREPARATION OF ELAFIBRANOR
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Paragraph 0122-0124, (2020/05/21)
The present invention provides a process for elafibranor, the process comprising reacting compound of formula II or the compound of formula III with a compound of formula IV. The present invention also involve purification of elafibranor by reacting elafi
DUAL-ACTION ELAFIBRANOR METFORMIN SALT FOR TREATING OBESITY ASSOCIATED WITH NON-ALCOHOLIC STEATOHEPATITIS (NASH) AND HYPERTRIGLYCERIDAEMIA
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Paragraph 0086-0100, (2020/02/13)
Drugs derived from elafibranor. One or more embodiments relate more particularly to a composition comprising at least one active principle, wherein the at least one active principle comprises an elafibranor metformin salt. One or more embodiments also rel
