DG172 dihydrochloride

目录号: HY-19737A 纯度: 99.03%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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

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DG172 dihydrochloride Chemical Structure

CAS No. : 1361504-77-9

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规格	价格	是否有货
10 mM * 1 mL in Water	￥770	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
25 mg	￥2400	In-stock
50 mg	￥3900	In-stock
100 mg	￥6300	In-stock
200 mg		询价
500 mg		询价

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PPARα PPARβ/δ PPARγ PPAR PPARδ

生物活性
实验参考方法
纯度 & 产品资料
参考文献

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].

MCE 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

性状

固体

颜色

Light yellow to yellow

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 中的溶解度 : 14.29 mg/mL (31.39 mM; 超声助溶)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.03%

选择批次：

Data Sheet (600 KB) SDS (251 KB)

COA (265 KB) LCMS (97 KB)

产品使用指南 (1538 KB)

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. [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]

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]. MCE 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. [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]

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].

MCE 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. [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]

DG172 dihydrochloride 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.1967 mL	10.9837 mL	21.9674 mL	54.9185 mL
	5 mM	0.4393 mL	2.1967 mL	4.3935 mL	10.9837 mL
	10 mM	0.2197 mL	1.0984 mL	2.1967 mL	5.4919 mL
	15 mM	0.1464 mL	0.7322 mL	1.4645 mL	3.6612 mL
	20 mM	0.1098 mL	0.5492 mL	1.0984 mL	2.7459 mL
	25 mM	0.0879 mL	0.4393 mL	0.8787 mL	2.1967 mL
	30 mM	0.0732 mL	0.3661 mL	0.7322 mL	1.8306 mL

* 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。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DG1721361504-77-9DG 172DG-172PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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DG172 dihydrochloride

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DG172 dihydrochloride 相关产品

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实验参考方法

纯度 & 产品资料

参考文献

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DG172 dihydrochloride 相关分类

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DG172 dihydrochloride

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DG172 dihydrochloride 相关抗体

DG172 dihydrochloride 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PPAR 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

DG172 dihydrochloride 相关抗体:

摩尔计算器

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DG172 dihydrochloride 相关分类

完整储备液配制表

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