Elafibranor(GFT505)
- Product Name
- Elafibranor(GFT505)
- CAS No.
- 923978-27-2
- Chemical Name
- Elafibranor(GFT505)
- Synonyms
- CS-2411;SureCN815512;elafibranor E;Elafibranor(GFT505);GFT505(ELAFIBRANOR);GFT505; GFT-505; GFT 505;;Elafibranor, 10 mM in DMSO;Elafibranor (GFT-505, Ph III);ELAFIBRANOR;GF T505;GFT-505;GFT505;Elafibranor(GFT505) ISO 9001:2015 REACH
- CBNumber
- CB43049684
- Molecular Formula
- C22H24O4S
- Formula Weight
- 384.49
- MOL File
- 923978-27-2.mol
Elafibranor(GFT505) Property
- 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.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 23508
- Product name
- Elafibranor
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 23508
- Product name
- Elafibranor
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 23508
- Product name
- Elafibranor
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
- Product number
- G368870
- Product name
- GFT-505
- Packaging
- 25mg
- Price
- $65
- Updated
- 2021/12/16
- Product number
- CS-5522
- Product name
- Elafibranor
- Purity
- 99.18%
- Packaging
- 5mg
- Price
- $72
- Updated
- 2021/12/16
Elafibranor(GFT505) Chemical Properties,Usage,Production
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.
Uses
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
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Raw materials
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View Lastest Price from Elafibranor(GFT505) manufacturers
- Product
- Elafibranor(GFT505) 923978-27-2
- Price
- US $8.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100MT
- Release date
- 2018-12-15