DG172 dihydrochloride 

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

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

455.22

C₂₀H₂₂BrCl₂N₃

1361504-77-9

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]