DG 172 dihydrochloride
Biological Activity
Potent PPARβ/δ inverse agonist (IC50 = 26.9 nM). Inhibits Angptl4 gene expression in mouse myoblasts (IC50 = 9.5 nM) in vitro. Also augments GM-CSF/IL-4-induced differentiation of mature dendritic cells from bone marrow cells in culture. Orally available.
Compound Libraries
DG 172 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 455.22 |
| Formula | C20H20BrN3.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1361504-77-9 |
| PubChem ID | 57342888 |
| InChI Key | SABUORLIDVBCPI-WTLOABTRSA-N |
| Smiles | BrC(C=CC=C1)=C1/C(C#N)=C/C2=CC=C(N3CCN(C)CC3)C=C2.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.52 | 100 | |
| water | 45.52 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 455.22. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.2 mL | 10.98 mL | 21.97 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.39 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.2 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lieber et al (2015) The inverse agonist DG172 triggers a PPARβ/δ-independent myeloid lineage shift and promotes GM-CSF/IL-4-induced dendritic cell differentiation. Mol.Pharmacol. 87 162 PMID: 25398837
Lieber et al (2012) (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. 55 2858 PMID: 22369181
If you know of a relevant reference for DG 172 dihydrochloride, please let us know.
View Related Products by Target
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Citations for DG 172 dihydrochloride
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