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。
| 生物活性 | Zunsemetinib (CDD-450) is an orally active and selectivep38αmitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1]. |
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体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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 IDcmice 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(194.58 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9458 mL | 9.7291 mL | 19.4583 mL | | 5 mM | 0.3892 mL | 1.9458 mL | 3.8917 mL | | 10 mM | 0.1946 mL | 0.9729 mL | 1.9458 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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