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Elafibranor (GFT505) (Synonyms: GFT505)

カタログ番号GC18151

Elafibranor (GFT505) (GFT505) は PPARα/δ です。それぞれ 45 および 175 nM の EC50 を持つアゴニスト。

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Elafibranor (GFT505) 化学構造

Cas No.: 923978-27-2

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$52.00
在庫あり
5mg
$47.00
在庫あり
10mg
$69.00
在庫あり
25mg
$163.00
在庫あり
50mg
$267.00
在庫あり
100mg
$404.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

GFT505 improves insulin sensitivity and early studies indicate it may be useful in non-alcoholic fatty liver disease which is being tested in a Phase IIb study1. 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 insulin sensitivity, glucose homeostasis, and lipid metabolism and reduces inflammation2. 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 GFT505. GFT505 does not induce cardiac adverse effects of PPARγ-activating agonists in monkeys3.

References:
1. Liu ZM, et al. Early investigational drugs targeting PPAR-α for the treatment of metabolic disease.Expert Opin Investig Drugs. 2015 May;24(5):611-21.
2. Ratziu V, et al. Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. Gastroenterology. 2016 May;150(5):1147-1159.
3. Hanf R, et al. 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.Diab Vasc Dis Res. 2014 No

Chemical Properties

Cas No. 923978-27-2 SDF
同義語 GFT505
Chemical Name (E)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoic acid
Canonical SMILES CSC1=CC=C(C(/C=C/C2=CC(C)=C(OC(C)(C)C(O)=O)C(C)=C2)=O)C=C1
Formula C22H24O4S M.Wt 384.49
溶解度 DMSO : ≥ 33 mg/mL (85.83 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6008 mL 13.0042 mL 26.0085 mL
5 mM 0.5202 mL 2.6008 mL 5.2017 mL
10 mM 0.2601 mL 1.3004 mL 2.6008 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Review for Elafibranor (GFT505)

Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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