Zunsemetinib T39126

Product Introduction
Bioactivity


英文名: Zunsemetinib

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: CDD 450 | ATI450 | CDD450 | ATI 450 | Zunsemetinib

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途