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. It inhibits the expression of IL-17 (at 0.5 uM) in nave 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. 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.
GSK805
目录号: GC18591纯度: >98%同义词: N-(2,6-二氯-2'-(三氟甲氧基)-[1,1'-联苯]-4-基)-2-(4-(乙基磺酰基)苯基)乙酰胺
An RORγt inverse agonist
Cas No.: 1426802-50-7
| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥540.00 | 现货 | 1 | |
| 5mg | ¥1,350.00 | 现货 | 1 | |
| 10mg | ¥2,160.00 | 现货 | 1 | |
| 25mg | ¥4,095.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,581.00 | 现货 | 1 |
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产品描述 Description
实验参考方法 Experimental Reference Method
Animal experiment: | Animal administration[1]GSK805 are orally administered once daily at 3 doses (1, 3, and 10 mg/kg) to EAE mice from the day of immunization. Compared to the control, the treatment with 9a or 9g resulted in a delay and significant reduction in clinical severity of EAE in a dose-dependent manner. Compared to thiazole ketone amide 2, which only showed EAE efficacy up to day 20 at 100 mg/kg twice daily dosing,32 the biaryl amides 9a and 9g are much more efficacious. This could be attributed to their good in vitro activities as well as much improved oral exposure and CNS penetration. However, it should be noted that although 9g had more brain exposure than 9a, it exhibited less efficacy than 9a in EAE experiments, indicating that there might be additional factors such as "free" brain concentration affecting in vivo efficacy[1]. |
References: [1]. Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors. ACS Med Chem Lett. 2015 May 26;6(7):787-792. |
产品文档 Product Documents
Purity:>98%
化学性质Chemical Properties
CAS 号
1426802-50-7
同义词
N-(2,6-二氯-2'-(三氟甲氧基)-[1,1'-联苯]-4-基)-2-(4-(乙基磺酰基)苯基)乙酰胺
化学名
N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)-benzeneacetamide
SMILES
ClC1=CC(NC(CC2=CC=C(S(CC)(=O)=O)C=C2)=O)=CC(Cl)=C1C3=C(OC(F)(F)F)C=CC=C3
分子式
C23H18Cl2F3NO4S
分子量
532.4 g/mol
溶解性
DMF: 3 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
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。
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。
计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度
g/mol