Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor.
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.
In vivo, Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing.
Molecular Weight | 513.92 |
Formula | C25H22ClF2N5O3 |
CAS Number | 1640282-42-3 |
Solubility (25°C) | DMSO 90 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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