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.
Molecular Weight | 416.86 |
Formula | C19H21ClN6O3 |
CAS Number | 1700693-08-8 |
Solubility (25°C) | DMSO 30 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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