Zunsemetinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Zunsemetinib (CDD-450) 是一种具有口服活性的 p38α 丝裂原激活蛋白激酶激活蛋白激酶2 (MK2)通路抑制剂。Zunsemetinib 可用于免疫炎症性疾病的研究。

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor.Zunsemetinib can be used for the research of immuno-inflammatory diseases.

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.Zunsemetinib (0.4 nM~1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability.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.RT-PCR 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.

Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing.Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density.Zunsemetinib prevents osteopenia in NOM IDc mice through inhibition of osteoclastogenesis.Animal Model:8-week-old WT female mice 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 Dosage:10 and 20 mg/kg Administration:P.o.Result:Increased bone density.

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MAPK/ERK Signaling

p38 MAPK

MAPK

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1640282-42-3

513.92

C25H22ClF2N5O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (194.58 mM; 超声助溶 )

Cc1cnc(cc1-n1c(C)cc(OCc2ncc(F)cc2F)c(Cl)c1=O)-c1ccnc(n1)C(C)(C)O

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(-20℃)

With Ice Pack

≥ 2 years