S82989 |
DG172 (dihydrochloride) |
源叶(MedMol) | 99% |
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- 产品描述: DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC50 of 27 nM
- 靶点: PPARβ/δ:27 nM (IC50);PPAR
- 体外研究:
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
- 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.
- 溶解性: Soluble in H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.197 ml 10.984 ml 21.967 ml 5 mM 0.439 ml 2.197 ml 4.393 ml 10 mM 0.22 ml 1.098 ml 2.197 ml 50 mM 0.044 ml 0.22 ml 0.439 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)