Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK805 是能够生物利用的、具有 CNS 穿透性的 RORγt 抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 513 | 现货 | ||
2 mg | ¥ 745 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,990 | 现货 | ||
25 mg | ¥ 3,990 | 现货 | ||
50 mg | ¥ 4,920 | 现货 | ||
100 mg | ¥ 6,990 | 现货 | ||
200 mg | ¥ 9,430 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,330 | 现货 |
产品描述 | GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding |
体外活性 | GSK805 inhibits the expression of IL-17 (at 0.5 μM) in na?ve CD4+ T cells activated under Th17-cell-polarizing conditions and affects the broader RORγt-dependent gene network, inhibiting the development and pathogenic function of Th17 cells[1]. |
体内活性 | GSK805 significantly reduces the severity of experimental autoimmune encephalomyelitis (EAE), a mouse model of multiple sclerosis, when given orally to the hosts at 10 mg/kg daily beginning at the time of disease induction[1]. |
细胞实验 | CD4+CD62LhighCD25? naive CD4+ T cells were purified by FACS sorting following a MACS bead isolation of CD4+ cells. Naive CD4+ cells were activated with plate-bound anti-CD3 (2 μg/ml) and anti-CD28 (2 μg/ml). For Th17 cell differentiation, cultures were supplemented with IL-6 (20 ng/ml) plus TGF-β1 (1 ng/ml), and IL-23 (10 ng/ml) was added after 48 h. RORγt inhibitors or vehicle control DMSO was also included in the cultures. After 96 h, cells were collected for further experiments[1]. |
分子量 | 532.36 |
分子式 | C23H18Cl2F3NO4S |
CAS No. | 1426802-50-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (187.84 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8784 mL | 9.3921 mL | 18.7843 mL | 46.9607 mL |
5 mM | 0.3757 mL | 1.8784 mL | 3.7569 mL | 9.3921 mL | |
10 mM | 0.1878 mL | 0.9392 mL | 1.8784 mL | 4.6961 mL | |
20 mM | 0.0939 mL | 0.4696 mL | 0.9392 mL | 2.348 mL | |
50 mM | 0.0376 mL | 0.1878 mL | 0.3757 mL | 0.9392 mL | |
100 mM | 0.0188 mL | 0.0939 mL | 0.1878 mL | 0.4696 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GSK805 1426802-50-7 Metabolism ROR GSK 805 immunity RAR-related orphan receptor Inhibitor inhibit oral CNS penetrant Th17 cell GSK-805 inhibitor