购物车
- 全部删除
- 您的购物车当前为空
GC376 sodium 是一种 3C 样蛋白酶 (3CLpro) 抑制剂,IC50 值范围为 0.49~4.35 μM。
为众多的药物研发团队赋能,
让新药发现更简单!
GC376 sodium 是一种 3C 样蛋白酶 (3CLpro) 抑制剂,IC50 值范围为 0.49~4.35 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 339 | 现货 | |
5 mg | ¥ 792 | 现货 | |
10 mg | ¥ 1,170 | 现货 | |
25 mg | ¥ 1,800 | 现货 | |
50 mg | ¥ 2,780 | 现货 | |
100 mg | ¥ 3,970 | 现货 | |
500 mg | ¥ 8,590 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 897 | 现货 |
产品描述 | GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM. |
靶点活性 | 3CLpro:0.49~4.35 μM. |
体外活性 | GC376对冠状病毒(TGEV、FIPV、MHV、229E和BCV)、卡利西病毒(NV和MNV-1)以及皮克纳病毒(HRVs 18、51和68、EV71和PTV)表现出显著的抑制效果,IC50值达到纳摩尔或低微摩尔水平,除了FCV和HAV外。有趣的是,FCV对GC376的敏感性较低,其IC50值为35 μM [1]。 |
体内活性 | GC376以15 mg/kg的剂量,每12小时通过皮下注射给药。结果表明,在初始治疗后的2周内,20只接受GC376治疗的猫中有19只恢复了正常健康状况。然而,疾病迹象在初次治疗后1-7周内复发,复发和新发病例最终需要至少治疗12周。在初次或重复治疗后的1-7周内,13只中的19只猫发生了不再对治疗有反应的复发 [2]。 |
细胞实验 | The toxic dose for 50% cell death (TD50) for each compound was determined for the various cells used in this study. Confluent cells grown in 96-well plates were treated with various concentrations (1 to 500 μM) of each compound for 72 h. Cell cytotoxicity was measured by a CytoTox 96 nonradioactive cytotoxicity assay kit and crystal violet staining. The in vitro therapeutic index was calculated by dividing the TD50 by the IC50 [1]. |
动物实验 | GC376 was synthesized in a highly pure form and formulated at a concentration of 53 mg/ml in 10% ethanol and 90% polyethylene glycol 400, as described previously. GC376 was administered subcutaneously (SC) at a dosage of 15 mg/kg q12h SC, unless stated otherwise. The effective dosage for cats with experimentally induced FIP was 10 mg/kg/ q12h SC, but the dosage was raised to 15 mg/kg after the first cat (CT01) failed to respond to a lower dose of 10 mg/kg suggested by earlier pharmacokinetic studies. This was a clinical decision based on this one cat's response to treatment [2]. |
分子量 | 507.53 |
分子式 | C21H30N3NaO8S |
CAS No. | 1416992-39-6 |
Smiles | [Na+].[H][C@@](CC1CCNC1=O)(NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1)C(O)S([O-])(=O)=O |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | 5% DMSO+95% Saline: 2.25 mg/mL (4.43 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO: 45 mg/mL (88.66 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容