GSK2881078
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ￥760.00 | 10-15工作日发货 | |
| 10mg | ￥1235.00 | 10-15工作日发货 | |
| 25mg | ￥2470.00 | 10-15工作日发货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
GSK2881078 is a potent and selective androgen receptor modulator (SARM) [1].
Steroidal nuclear receptor (NR) ligands play important roles in the health of both men and women. Dihydrotestosterone (DHT) and testosterone (T) are endogenous steroidal ligands for the androgen receptor (AR) that play a role in every tissue type found in the mammalian body. During the development of the fetus, androgens play an important role in sexual differentiation and development of male sexual organs. SARMs are small molecule pharmacotherapeutics that have the potential to afford the important benefits of androgen therapy without the undesired side-effects [1].
GSK2881078 is a potent and selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. GSK2881078 is currently in phase I clinical trials [1].
Reference:
[1]. https://newdrugapprovals.org/2016/06/14/gsk-2881078/
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 1539314-06-1 |
| 分子式 | C14H13F3N2O2S |
| 分子量 | 330.3 |
| 小分子别名 | GSK-2881078 |
| 化学名称 | 1-[(1R)-1-methyl-2-(methylsulfonyl)ethyl]-4-(trifluoromethyl)-1H-indole-5-carbonitrile |
| 溶解度 | ≤20mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
| SMILES | C[C@H](CS(C)(=O)=O)[n](cc1)c(cc2)c1c(C(F)(F)F)c2C#N |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | GSK-2881078是一种口服活性非甾体选择性雄激素受体调节剂（SARM），在雄激素组织中作为部分AR激动剂，而在合成代谢组织中主要作为完全AR激动剂，可诱导PC3（AR）2细胞中AR介导的转录激活（EC50 = 3.99 nM），非甾体AR拮抗剂比卡鲁胺（Bicalutamide）可抑制该效应。GSK-2881078 可用于研究与慢性和急性疾病相关的肌无力和恶病质。 |
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