同义名 :	DG-172 (hydrochloride); DG172 dihydrochloride; DG-172
	CAS号 :	1361504-77-9
	货号 :	A545888
	分子式 :	C20H22BrCl2N3
	纯度 :	99%+
	分子量 :	455.22
	MDL号 :	MFCD29924728
	存储条件：	Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

DG172 dihydrochloride functions as a selective antagonist of PPARβ/δ, showing an IC50 of 27 nM. It bolsters the recruitment of transcriptional corepressors and diminishes the transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts, with an IC50 of 9.5 nM[1]. At a concentration of 1 µM, DG172 encourages the differentiation of dendritic cells (DCs) from GM-CSF-induced mouse bone marrow cells (BMCs), concurrently reducing the presence of Ly6b+/Gr1+ granulocytic cells. It also influences the transcriptome of GM-CSF differentiated BMCs from both WT and Ppard-null mice, pinpointing its action to a specific phase of GM-CSF-induced differentiation[2]. Furthermore, DG172, in doses of 0.1 and 1.0 µM, dose-dependently augments the proliferation of TM4 cells while lowering the expression of claudin-11[3].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.20mL 0.44mL 0.22mL	10.98mL 2.20mL 1.10mL	21.97mL 4.39mL 2.20mL

参考文献

[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.