DG 172 dihydrochloride

Discontinued Product

DG 172 dihydrochloride (Cat. No. 5566) has been withdrawn from sale for commercial reasons.
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)
Literature (3)

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
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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Citations for DG 172 dihydrochloride

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