GW-870086
目录号: PL01445 纯度: ≥98%
GW-870086 是一种有效的抗炎剂,为糖皮质激素受体 (glucocorticoid receptor) 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
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中文名称
GW-870086
英文名称
GW-870086
英文别名
cyanomethyl (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(2,2,3,3-tetramethylcyclopropanecarbonyl)oxy-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phe;(6S,8S,9R,10S,11S,13S,14S,16R,17R)-cyanomethyl 6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-((2,2,3,3-tetramethylcyclopropanecarbonyl)oxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate;cyanomethyl (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(2,2,3,3-tetramethylcyclopropanecarbonyl)oxy-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthrene-;GSK870086;GW870086;GW-870086X;O891A2A3ZU;AMY16811;GW870086X;DB12322;Q27285471;Androsta-1,4-diene-17-carboxylic acid, 6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-(((2,2,3,3-tetrame
Cas No.
827319-43-7
分子式
C31H39F2NO6
分子量
559.64
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GW-870086 是一种有效的抗炎剂,为糖皮质激素受体 (glucocorticoid receptor) 激动剂,在 A549 细胞中,抑制 NFκB 报告基因活性,pIC50 值为 10.1。
生物活性
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC 50 of 10.1 in A549 cells expressing NF-κB.
性状
Solid
IC50 & Target[1][2]
pIC50: 10.1 (glucocorticoid receptor, A549 NF-κB cells)
体外研究(In Vitro)
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). 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (178.69 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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