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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
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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).
pka
3.30±0.11(Predicted)
form 
solid
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.
InChI
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+
InChIKey
AFLFKFHDSCQHOL-IZZDOVSWSA-N
SMILES
C(O)(=O)C(OC1=C(C)C=C(/C=C/C(C2=CC=C(SC)C=C2)=O)C=C1C)(C)C
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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.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23508
Product name
Elafibranor
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23508
Product name
Elafibranor
Purity
≥98%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
23508
Product name
Elafibranor
Purity
≥98%
Packaging
10mg
Price
$184
Updated
2024/03/01
TRC
Product number
G368870
Product name
GFT-505
Packaging
25mg
Price
$65
Updated
2021/12/16
ChemScene
Product number
CS-5522
Product name
Elafibranor
Purity
99.18%
Packaging
5mg
Price
$72
Updated
2021/12/16
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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.

in vivo

Elafibranor is well tolerated and does not cause weight gain or cardiac events, but does produce a mild, reversible increase in serum creatinine. Elafibranor improves glucose homeostasis, and lipid metabolism and reduces inflammation[2]. Elafibranor (GFT505) treatment improves glucose control and plasma lipids in diabetic db/db mice. A significant dose-dependent reduction of hepatic expression of the key gluconeogenic enzymes glucose 6-phosphatase (G6Pase), PEPCK, and fructose 1,6-bisphosphatase 1 (FBP1) is observed with Elafibranor. Elafibranor does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys[3].

IC 50

PPAR-α: 45 nM (EC50); PPAR-δ: 175 nM (EC50)

References

[1] BERTRAND CARIOU. Effects of the new dual PPAR α/δ agonist GFT505 on lipid and glucose homeostasis in abdominally obese patients with combined dyslipidemia or impaired glucose metabolism.[J]. Diabetes Care, 2011, 34 9: 2008-2014. DOI:10.2337/dc11-0093
[2] BERTRAND CARIOU. Dual peroxisome proliferator-activated receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.[J]. Diabetes Care, 2013, 36 10: 2923-2930. DOI:10.2337/dc12-2012
[3] RÉMY HANF. The dual peroxisome proliferator-activated receptor alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.[J]. Diabetes & Vascular Disease Research, 2014, 11 6: 440-447. DOI:10.1177/1479164114548027
[4] BART STAELS. Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha/delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis[J]. Hepatology, 2013, 58 6: 1941-1952. DOI:10.1002/hep.26461
[5] VLAD RATZIU . Elafibranor, an Agonist of the Peroxisome Proliferator−Activated Receptor−α and −δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening[J]. Gastroenterology, 2016, 150 5: Pages 1147-1159.e5. DOI:10.1053/j.gastro.2016.01.038
[6] JOOST BOECKMANS . Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH[J]. Pharmacological research, 2019, 144: Pages 377-389. DOI:10.1016/j.phrs.2019.04.016

Elafibranor(GFT505) Preparation Products And Raw materials

Raw materials

Preparation Products

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Elafibranor(GFT505) Suppliers

China 131 India 2 United Kingdom 1 United States 11 Global 145
Nanjing YakeLun Pharmaceutical Co., Ltd.
Tel
025-66096098 3165145969
Fax
QQ3165145969
Email
sales@accoronpharm.com
Country
China
ProdList
3924
Advantage
55
Changzhou Chenhong Biotechnology Co., Ltd.
Tel
+86-0519-85788828 +86-13775037613
Email
sales@chemrenpharm.com
Country
China
ProdList
3934
Advantage
58
Nantong Hanfang Biotechnology Co. , Ltd.
Tel
hanfangpharma@126.com; 18616537568
Email
hanfangpharma@126.com
Country
China
ProdList
29965
Advantage
58
Changsha Fuzhen Biotechnology Co.，LTD
Tel
0731-13823398 15111215862
Email
313359644@qq.com
Country
China
ProdList
4161
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6003
Advantage
61
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1077
Advantage
64
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
Beijing Yisiyan Technology Research Center
Tel
010-56645598 13366904824
Fax
01062230033
Email
bjkaida@163.com
Country
China
ProdList
1618
Advantage
59
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
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61
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View Lastest Price from Elafibranor(GFT505) manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Elafibranor 923978-27-2
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2025-09-09
Wuhan JiyunZen Tech Co., Ltd.
Product
Elafibranor 923978-27-2
Price
US $5.00-0.50/KG
Min. Order
1KG
Purity
99% hplc
Supply Ability
500TONS
Release date
2025-06-05
Career Henan Chemical Co
Product
Elafibranor(GFT505) 923978-27-2
Price
US $8.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100MT
Release date
2018-12-15

923978-27-2, Elafibranor(GFT505)Related Search:

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