DG172 dihydrochloride

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DG172 dihydrochloride  纯度: 99.03%

DG172 dihydrochloride 是一种选择性的 PPARβ/δ 拮抗剂，IC50 值为 27 nM。

DG172 dihydrochloride

DG172 dihydrochloride Chemical Structure

CAS No. : 1361504-77-9

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10 mM * 1 mL in Water ￥1155 In-stock
5 mg ￥1050 In-stock
10 mg ￥1600 In-stock
50 mg ￥6400 In-stock
100 mg ￥11000 In-stock
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生物活性

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

IC50 & Target[1]

PPARβ/δ

27 nM (IC50)

体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

455.22

Formula

C20H22BrCl2N3
CAS 号

1361504-77-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

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

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1967 mL 10.9837 mL 21.9674 mL
5 mM 0.4393 mL 2.1967 mL 4.3935 mL
10 mM 0.2197 mL 1.0984 mL 2.1967 mL

*

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。
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.
Cell Assay
[3]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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.

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