DG172 dihydrochloride

DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.

Product information

CAS Number: 1361504-77-9

Molecular Weight: 455.22

Formula: C20H22BrCl2N3

Chemical Name: (2Z)-2-(2-bromophenyl)-3-[4-(4-methylpiperazin-1-yl)phenyl]prop-2-enenitrile; bis(chlorohydrogen)

Smiles: Cl.Cl.CN1CCN(CC1)C1C=CC(/C=C(\C#N)/C2=CC=CC=C2Br)=CC=1

InChiKey: SABUORLIDVBCPI-WTLOABTRSA-N

InChi: 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+;;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 14.29 mg/mL (31.39 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM. DG172 enhances transcriptional corepressor recruitment, and down-regulates transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts (IC50, 9.5 nM). DG172 (1 µM) promotes the differentiation of dendritic cells (DCs) from GM-CSF-induced mouse bone marrow cells (BMCs) and reduces Ly6b+/Gr1+ granulocytic cells. DG172 has effects on the transcriptome of GM-CSF differentiated BMCs from WT and Ppard null mice, and acts at a specific stage of GM-CSF-induced differentiation. DG172 (0.1, 1.0 µM) dose-dependently promotes proliferation of TM4 cells. DG172 reduces expression of claudin-11 in TM4 cells.

References:

1. Lieber S, 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. 2012 Mar 22;55(6):2858-68.
2. Lieber S, 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. 2015 Feb;87(2):162-73.
3. Yao PL, et al. Peroxisome Proliferator-activated Receptor-D (PPARD) Coordinates Mouse Spermatogenesis by Modulating Extracellular Signal-regulated Kinase (ERK)-dependent Signaling. J Biol Chem. 2015 Sep 18;290(38):23416-31.

Products are for research use only. Not for human use.