DG 172 dihydrochloride

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Cat.No. 5566 - DG 172 dihydrochloride | C20H20BrN3.2HCl | CAS No. 1361504-77-9
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)
Datasheet
Citations
Reviews
Literature

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

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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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 45.52 100
DMSO 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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References

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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