JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM.
In vitro: At a concentration of 1 μM, JH-II-127 only inhibited the kinase activities of SmMLCK and CHK2 to greater than 90% of the DMSO control (complete results presented in the Supporting Information). Dose–response analysis revealed inhibition of SmMLCK with an IC50 = 81.3 nM and CHK2 with an IC50 = 27.6 nM.
In vivo: JH-II-127 can inhibit phosphorylation of Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 30 mg/kg.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 30 mg/mL|
Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor.
Hatcher JM, et al. ACS Med Chem Lett. 2015 Apr 7;6(5):584-9. PMID: 26005538.
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