An orally available PPARβ/δ inverse agonist
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DG-172 (hydrochloride)

Item No. 19128

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-bromo-αZ-[[4-(4-methyl-1-piperazinyl)phenyl]methylene]-benzeneacetonitrile, dihydrochloride
CAS Number
1361504-77-9
Molecular Formula
C20H20BrN3 • 2HCl
Formula Weight
455.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
λmax
241, 348 nm
SMILES
CN1CCN(C2=CC=C(/C=C(C#N)/C3=C(Br)C=CC=C3)C=C2)CC1.Cl.Cl
InChi Code
InChI=1S/C20H20BrN3.2ClH/c1-23-10-12-24(13-11-23)18-8-6-16(7-9-18)14-17(15-22)19-4-2-3-5-20(19)21;;/h2-9,14H,10-13H2,1H3;2*1H/b17-14+;;
InChi Key
SABUORLIDVBCPI-WTLOABTRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Product Description

    DG-172 is an orally available inverse agonist of PPARβ/δ (IC50 = 27 nM), down-regulating transcription of ANGPTL4 in mouse myoblasts (IC50 = 9.5 nM).1 It alters the differentiation of bone marrow cells, augmenting GM-CSF-induced development into subsets of mature and immature dendritic cells.2 Inverse agonists of PPARβ/δ, including DG-172, inhibit cancer cell invasion through suppression of ANGPTL4 expression.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lieber, S., Scheer, F., Meissner, W., 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. 55(6), 2858-2868 (2012).

    2. Lieber, S., Scheer, F., Finkernagel, F., 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. 87(2), 162-173 (2015).

    3. Adhikary, T., Brandt, D.T., Kaddatz, K., et al. Inverse PPARβ/δ agonists suppress oncogenic signaling to the ANGPTL4 gene and inhibit cancer cell invasion. Oncogene 32(44), 5241-5252 (2013).