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Submit ReviewDG 172 dihydrochloride
Description: Potent PPARβ/δ inverse agonist; promotes BMC differentiation
Chemical Name: (αZ)-2-Bromo-α-[[4-(4-methyl-1-piperazinyl)phenyl]methylene]benzeneacetonitrile dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for DG 172 dihydrochloride
DG 172 dihydrochloride is a 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.
Technical Data for DG 172 dihydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for DG 172 dihydrochloride
References for DG 172 dihydrochloride
References are publications that support the biological activity of the product.
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
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