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 (GFT-505, Ph III);ELAFIBRANOR;GF T505;GFT-505;GFT505;Elafibranor(GFT505) ISO 9001:2015 REACH;Propanoic acid, 2-[2,6-dimethyl-4-[(1E)-3-[4-
- CBNumber:
- CB43049684
- Molecular Formula:
- C22H24O4S
- Molecular Weight:
- 384.49
- MDL Number:
- MOL File:
- 923978-27-2.mol
Boiling point | 569.0±50.0 °C(Predicted) |
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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. |
FDA UNII | 2J3H5C81A5 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P305+P351+P338 | |||||||||
NFPA 704 |
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Elafibranor(GFT505) price More Price(11)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 23508 | Elafibranor ≥98% | 923978-27-2 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 23508 | Elafibranor ≥98% | 923978-27-2 | 5mg | $116 | 2024-03-01 | Buy |
Cayman Chemical | 23508 | Elafibranor ≥98% | 923978-27-2 | 10mg | $184 | 2024-03-01 | Buy |
TRC | G368870 | GFT-505 | 923978-27-2 | 25mg | $65 | 2021-12-16 | Buy |
ChemScene | CS-5522 | Elafibranor 99.18% | 923978-27-2 | 5mg | $72 | 2021-12-16 | Buy |
Elafibranor(GFT505) Chemical Properties,Uses,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
Elafibranor(GFT505) Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ENBRIDGE PHARMTECH CO., LTD. | +8613812269233 | tinayang@enbridgepharm.com | China | 303 | 58 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 | product@chemlin.com.cn | CHINA | 3012 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
Shandong chuangyingchemical Co., Ltd. | 18853181302 | sale@chuangyingchem.com | CHINA | 5909 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
Shaanxi Dideu Medichem Co. Ltd | +86-029-81148696 +8615536356810 | 1047@dideu.com | China | 3255 | 58 |
Wuxi Rejoys chemical Technology Co., Ltd. | 0510-86103381 | sales@rejoyschem.com | CHINA | 976 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29067 | 58 |
View Lastest Price from Elafibranor(GFT505) manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2020-01-03 | Elafibranor(GFT505)
923978-27-2
|
US $0.10 / KG | 1KG | 99.0% | 1000 tons | Shaanxi Dideu Medichem Co. Ltd | ||
2019-07-06 | Elafibranor(GFT505)
923978-27-2
|
US $8.00 / kg | 1kg | 99% | 100MT | Career Henan Chemical Co |
- Elafibranor(GFT505)
923978-27-2
- US $0.10 / KG
- 99.0%
- Shaanxi Dideu Medichem Co. Ltd
- Elafibranor(GFT505)
923978-27-2
- US $8.00 / kg
- 99%
- Career Henan Chemical Co