Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK199 是可逆的 PAD4选择性抑制剂,当缺少钙离子时,其 IC50值为 200 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 987 | 现货 | ||
2 mg | ¥ 1,490 | 现货 | ||
5 mg | ¥ 2,390 | 现货 | ||
10 mg | ¥ 3,990 | 现货 | ||
25 mg | ¥ 6,280 | 现货 | ||
50 mg | ¥ 8,490 | 现货 | ||
100 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,790 | 现货 |
产品描述 | GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium). |
靶点活性 | PAD4:200 nM |
体内活性 | GSK199, in the murine collagen-induced arthritis model of rheumatoid arthritis. Mice were dosed daily from the time of collagen immunization with GSK199. Efficacy was assessed against a wide range of end-points, including clinical disease scores, joint histology and immunohistochemistry, serum and joint citrulline levels and quantification of synovial autoantibodies using a proteomic array containing joint peptides. Administration of GSK199 at 30 mg/kg led to significant effects on arthritis, assessed both by global clinical disease activity and by histological analyses of synovial inflammation, pannus formation and damage to cartilage and bone. In addition, significant decreases in complement C3 deposition in both synovium and cartilage were observed robustly with GSK199 at 10 mg/kg. Neither the total levels of citrulline measurable in joint and serum, nor levels of circulating collagen antibodies, were affected significantly by treatment with GSK199 at any dose level. In contrast, a subset of serum antibodies reactive against citrullinated and non-citrullinated joint peptides were reduced with GSK199 treatment. |
分子量 | 468.98 |
分子式 | C24H29ClN6O2 |
CAS No. | 1549811-53-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11 mg/mL (23.45 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1323 mL | 10.6614 mL | 21.3229 mL | 53.3072 mL |
5 mM | 0.4265 mL | 2.1323 mL | 4.2646 mL | 10.6614 mL | |
10 mM | 0.2132 mL | 1.0661 mL | 2.1323 mL | 5.3307 mL | |
20 mM | 0.1066 mL | 0.5331 mL | 1.0661 mL | 2.6654 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。
GSK199 1549811-53-1 Chromatin/Epigenetic PAD GSK 199 Inhibitor Peptidylarginine Deiminase GSK-199 Protein Arginine Deiminase inhibit inhibitor