DG172 dihydrochloride
Based on 1 publication(s) in Google Scholar
DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 1361504-77-9
- Formula: C20H22BrCl2N3
- Molecular Weight:455.22
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Obesity Compound Library
HY-L087
-
Transcription Factor-Targeted Library
HY-L090
-
Targeted Diversity Library
HY-L099
-
Nuclear Receptor Compound Library
HY-L126
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) DG172 dihydrochloride
More
Biological Activity
|
PPARβ/δ 27 nM (IC50) |
DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM. DG172 enhances transcriptional corepressor recruitment, and down-regulates transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts (IC50, 9.5 nM)[1]. DG172 (1 μM) promotes the differentiation of dendritic cells (DCs) from GM-CSF-induced mouse bone marrow cells (BMCs) and reduces Ly6b+/Gr1+ granulocytic cells. DG172 has effects on the transcriptome of GM-CSF differentiated BMCs from WT and Ppard null mice, and acts at a specific stage of GM-CSF-induced differentiation[2]. DG172 (0.1, 1.0 μM) dose-dependently promotes proliferation of TM4 cells. DG172 reduces expression of claudin-11 in TM4 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1361504-77-9
-
Appearance Solid
-
Molecular Weight 455.22
-
Formula C20H22BrCl2N3
-
Color Light yellow to yellow
-
SMILES
BrC(C=CC=C1)=C1/C(C#N)=C/C(C=C2)=CC=C2N3CCN(C)CC3.[H]Cl.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Cells
The Role of PPARβ/δ-Related Lipid Metabolism in High-Altitude Adaptation of Yak Coat Based on Proteomics and Metabolomics. [Abstract]2025 Nov 22;14(23):1843. PMID: 41369331
Solvent & Solubility
H2O : 14.29 mg/mL (31.39 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
The xCELLigence system is used for determining the changes in real time cell proliferation in response to activation of PPARD with an agonist (GW0742) or an inverse agonist (DG172) or the effect of inhibiting ERK signaling in TM4 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (275 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Lieber S, et al. (Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172): an orally bioavailable PPARβ/δ-selective ligand with inverse agonistic properties. J Med Chem. 2012 Mar 22;55(6):2858-68. [Content Brief]
[2]. Lieber S, et al. The inverse agonist DG172 triggers a PPARβ/δ-independent myeloid lineage shift and promotes GM-CSF/IL-4-induced dendritic cell differentiation. Mol Pharmacol. 2015 Feb;87(2):162-73. [Content Brief]
[3]. Yao PL, et al. Peroxisome Proliferator-activated Receptor-D (PPARD) Coordinates Mouse Spermatogenesis by Modulating Extracellular Signal-regulated Kinase (ERK)-dependent Signaling. J Biol Chem. 2015 Sep 18;290(38):23416-31. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1967 mL | 10.9837 mL | 21.9674 mL | 54.9185 mL |
| 5 mM | 0.4393 mL | 2.1967 mL | 4.3935 mL | 10.9837 mL | |
| 10 mM | 0.2197 mL | 1.0984 mL | 2.1967 mL | 5.4919 mL | |
| 15 mM | 0.1464 mL | 0.7322 mL | 1.4645 mL | 3.6612 mL | |
| 20 mM | 0.1098 mL | 0.5492 mL | 1.0984 mL | 2.7459 mL | |
| 25 mM | 0.0879 mL | 0.4393 mL | 0.8787 mL | 2.1967 mL | |
| 30 mM | 0.0732 mL | 0.3661 mL | 0.7322 mL | 1.8306 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DG172 dihydrochloride Related Classifications
HY-19737A Related Classifications
Powered by Bioz