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HomeProduct name listElafibranor(GFT505)

Elafibranor(GFT505)

  • CAS NO.:923978-27-2
  • Empirical Formula: C22H24O4S
  • Molecular Weight: 384.49
  • Update Date: 2024-11-09 19:38:33
Elafibranor(GFT505) Structural

What is Elafibranor(GFT505)?

Description

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, PLIN2, 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.

The Uses of Elafibranor(GFT505)

GFT-505 is a?dual?PPARα/δ agonist. Studies have shown that GFT-505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects. It may also be a potential new drug candidate for treating lipid and glucose disorders.

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

Properties of Elafibranor(GFT505)

Boiling point: 569.0±50.0 °C(Predicted)
Density  1.21±0.1 g/cm3(Predicted)
storage temp.  -20°
solubility  Soluble in DMSO (up to at least 25 mg/ml).
form  solid
pka 3.30±0.11(Predicted)
color  Pale yellow
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

Safety information for Elafibranor(GFT505)

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for Elafibranor(GFT505)

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