Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GLPG2534 是一种具有口服活性、选择性和有效性的 IRAK4 抑制剂,具有抗炎活性。GLPG2534 对人和小鼠 IRAK4 具有抑制作用,可用于研究银屑病和特应性皮炎。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,280 | 现货 | ||
5 mg | ¥ 2,820 | 现货 | ||
10 mg | ¥ 4,570 | 现货 | ||
25 mg | ¥ 6,920 | 现货 | ||
50 mg | ¥ 9,520 | 现货 | ||
100 mg | ¥ 12,800 | 现货 |
产品描述 | GLPG2534 is an orally active, selective and potent IRAK4 inhibitor with anti-inflammatory activity. GLPG2534 inhibits human and mouse IRAK4 and could be used to study psoriasis and atopic dermatitis. |
靶点活性 | IL-1β:55 nM, IRAK1:179 nM, mIRAK4:3.5 nM, hIRAK4:6.4 nM |
体外活性 | GLPG2534 inhibits IL-6 release driven by IL-1β with an IC50 of 55 nM[1]. It also inhibits TNF-α-driven IL-6 release, with an IC50 of 6.6 μM[1]. When applied at concentrations ranging from 0.1 to 10 μM for 16 hours, GLPG2534 inhibits the expression of S100A7, DEFB4A, CXCL8, and TNF in ciliated epithelial cells stimulated with ciliogenesis-promoting factors[1]. |
体内活性 | GLPG2534, administered orally at doses ranging from 0.3 to 10 mg/kg, inhibits CL097-driven TNF-α release in mouse blood[1]. Furthermore, oral administration of GLPG2534 at doses of 10 and 30 mg/kg, twice daily, alleviates inflammation in a psoriasis-like mouse model[1]. Additionally, GLPG2534, at doses of 3-30 mg/kg, orally administered twice daily for 5 days, mitigates the development of IL-33 and MC903-induced atopic dermatitis-like skin inflammation in mice[1]. |
别名 | GLPG-2534 |
分子量 | 424.45 |
分子式 | C21H24N6O4 |
CAS No. | 2095615-97-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL (188.48 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.356 mL | 11.78 mL | 23.5599 mL | 58.8998 mL |
5 mM | 0.4712 mL | 2.356 mL | 4.712 mL | 11.78 mL | |
10 mM | 0.2356 mL | 1.178 mL | 2.356 mL | 5.89 mL | |
20 mM | 0.1178 mL | 0.589 mL | 1.178 mL | 2.945 mL | |
50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.178 mL | |
100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.589 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。
GLPG2534 2095615-97-5 Immunology/Inflammation NF-Κb IRAK GLPG-2534 Inhibitor inhibitor inhibit