GW-870086
目录号 : GC31936
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
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 827319-43-7 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO : 100 mg/mL (178.69 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7869 mL | 8.9343 mL | 17.8686 mL |
| 5 mM | 0.3574 mL | 1.7869 mL | 3.5737 mL |
| 10 mM | 0.1787 mL | 0.8934 mL | 1.7869 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet