Elafibranor (GFT505) (Synonyms: GFT505) |
Catalog No.GC18151 |
Elafibranor (GFT505) (GFT505) es un PPARα/δ agonista con EC50 de 45 y 175 nM, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 923978-27-2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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
Cas No. | 923978-27-2 | SDF | |
Sinónimos | 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 |
Solubility | 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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
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. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 22 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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