Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zunsemetinib (CDD-450) is a potent and specific inhibitor of the p38α-MK2 pathway, exerting its effects through oral administration. It has proven activity against immuno-inflammatory diseases, making it a valuable tool for research in this area.
产品描述 | Zunsemetinib (CDD-450) is a potent and specific inhibitor of the p38α-MK2 pathway, exerting its effects through oral administration. It has proven activity against immuno-inflammatory diseases, making it a valuable tool for research in this area. |
体外活性 | Zunsemetinib (1 and 10 μM; 1 hour; WT and NOM ID BMMs) has no effect on NLRP3 expression, but decreases IL-1β expression by promoting IL-1β mRNA degradation[1]. Zunsemetinib (0.4 nM~1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability[1]. Zunsemetinib selectively blocks p38α MAPK activation of the proinflammatory kinase MK2 while sparing p38α activation of other effectors such as PRAK and ATF2. Zunsemetinib inhibits in vitro osteoclast formation induced by RANKL[1]. RT-PCR[1]Cell Line: WT and NOM ID BMMs Concentration: 1 and 10 μM Incubation Time: 1 hour Result: Had no effect on NLRP3 expression, but decreased IL-1β expression by promoting IL-1β mRNA degradation. |
体内活性 | Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing[1]. Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density[1]. Zunsemetinib prevents osteopenia in NOM ID c mice through inhibition of osteoclastogenesis[1]. Animal Model: 8-week-old WT female mice[1]Dosage: 1,000 ppm Administration: P.o. Result: Blocked LPS-induced TNF-α expression persisted for up to 4 weeks after dosing. Animal Model: Rats[1]Dosage: 10 and 20 mg/kg Administration: P.o. Result: Increased bone density. |
别名 | CDD-450, ATI-450 |
分子量 | 513.93 |
分子式 | C25H22ClF2N5O3 |
CAS No. | 1640282-42-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
Zunsemetinib 1640282-42-3 CDD 450 ATI450 CDD450 CDD-450 ATI-450 ATI 450 Inhibitor inhibitor inhibit