LRRK2-IN-1 is a cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor. IC50 is 13 nM, 6 nM, and 2.45 μM for wild type, G2019S mutant, and compound resistant A2016T mutant LRRK2, respectively.
|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 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.
|Solubility||100 mM in DMSO|
|Related LRRK2 Products|
MLi-2 is a highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).
PFE-360, also known as PF-06685360, is a potent and selective, brain penetrated inhibitor of LRRK2 kinase.
CZC 25146 is a potent LRRK2 inhibitor.
JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM.
GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
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