GW-870086

目录号: GC31936纯度: >98.00%

GW-870086是一种有效的抗炎剂，为糖皮质激素受体(glucocorticoidreceptor)激动剂，在A549细胞中，抑制NFκB报告基因活性，pIC50值为10.1。

Cas No.: 827319-43-7

规格	价格	库存	数量
5mg	¥493.00	现货	1
10mg	¥745.00	现货	1
25mg	¥1,426.00	现货	1
50mg	¥2,138.00	现货	1
100mg	¥3,208.00	现货	1
10mM (in 1mL DMSO)	¥608.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC50 of 10.1 in A549 cells expressing NF-κB.

GW-870086 a glucocorticoid receptor agonist, inhibits NFkB reporter gene with a pIC50 of 10.1, but shows no effect on the MMTV reporter genes in A549 cells, and has little or no activity at the oestrogen receptor, progesterone receptor, progesterone receptor, mineralocorticoid receptor or androgen receptor. GW-870086 (1 pM-1 μM) dose-dependently inhibits the L-6 release induced by TNF-α in A549 epithelial carcinoma cells and by IL-1 in MG63 osteosarcoma cells (pIC50s, 9.6, 10.2)[1]. GW-870086 (GW870086X; 10-100 nM) significantly increases fibronectin secretion. However, GW-870086 has no effect on MMP2 secretion, and does not increase cellular myocilin[2].

[1]. Uings IJ, et al. Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile. Br J Pharmacol. 2013 Jul;169(6):1389-403. [2]. Stamer WD, et al. Unique response profile of trabecular meshwork cells to the novel selective glucocorticoid receptor agonist, GW870086X. Invest Ophthalmol Vis Sci. 2013 Mar 1;54(3):2100-7.

实验参考方法 Experimental Reference Method

Cell experiment:

Cells are exposed to DEX, PRED, or GW-870086 at 0, 1, 3, 10, 30, 100 or 300 nM for 5 days. Compounds (GW-870086, etc.) are reconstituted in DMSO as 300-mM stock solutions that are diluted to give final drug concentrations in DMEM. Media (DMEM supplemented with 1% FBS) is changed after 48 hours and equal volumes of media from each group are collected after the final 72 hours of treatment, concentrated (×10), and added to an equal volume of ×2 sample buffer. Cells are then rinsed with PBS and scraped directly into 100-μL ×2 sample buffer/well. All samples are incubated at 100°C for 8 minutes and stored at −20°C until analysis[1].

References:

[1]. Uings IJ, et al. Discovery of GW870086: a potent anti-inflammatory steroid with a unique pharmacological profile. Br J Pharmacol. 2013 Jul;169(6):1389-403.
[2]. Stamer WD, et al. Unique response profile of trabecular meshwork cells to the novel selective glucocorticoid receptor agonist, GW870086X. Invest Ophthalmol Vis Sci. 2013 Mar 1;54(3):2100-7.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号

827319-43-7

SMILES

O=C(C1C(C)(C)C1(C)C)O[C@]2([C@@]3([C@@]([C@@]4([H])[C@@](F)([C@@]5(C([C@@H](F)C4)=CC(C=C5)=O)C)[C@@H](O)C3)([H])C[C@H]2C)C)C(OCC#N)=O

分子式

C₃₁H₃₉F₂NO₆

分子量

559.64 g/mol

溶解性

DMSO : 100 mg/mL (178.69 mM; Need ultrasonic)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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