DC Chemicals Limited
China
Product Name: DG-172 dihydrochloride
Price: $80.0/10mg $312.0/50mg $536.0/100mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: DG172 (dihydrochloride)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1361504-77-9

1361504-77-9 structure

1361504-77-9 structure

Name: DG 172 2HCl
Chemical Name: DG172 dihydrochloride
CAS Number: 1361504-77-9
Molecular Formula: C₂₀H₂₂BrCl₂N₃
Molecular Weight: 455.219
Catalog: Research Areas Cancer
Create Date: 2018-02-16 15:30:49
Modify Date: 2024-01-13 11:59:02
DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.

Name	DG172 dihydrochloride
Synonyms	(2Z)-2-(2-Bromophenyl)-3-[4-(4-methyl-1-piperazinyl)phenyl]acrylonitrile dihydrochloride Benzeneacetonitrile, 2-bromo-α-[[4-(4-methyl-1-piperazinyl)phenyl]methylene]-, (αZ)-, hydrochloride (1:2) DG172 (dihydrochloride)

Description	DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM.
Related Catalog	Research Areas >> Cancer
Target	PPARβ/δ:27 nM (IC50)
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)[1]. 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[2]. DG172 (0.1, 1.0 µM) dose-dependently promotes proliferation of TM4 cells. DG172 reduces expression of claudin-11 in TM4 cells[3].
Cell Assay	The xCELLigence system is used for determining the changes in real time cell proliferation in response to activation of PPARD with an agonist (GW0742) or an inverse agonist (DG172) or the effect of inhibiting ERK signaling in TM4 cells[3].
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.

Molecular Formula	C₂₀H₂₂BrCl₂N₃
Molecular Weight	455.219
Exact Mass	453.037415
Storage condition	2-8℃