Chemical Structure : MK-1468
CAS No.:
2769107-89-1
MK-1468
(MK1468)
Catalog No.: PC-21271Not For Human Use, Lab Use Only.
MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.
MK-1468 demonstrates near-equipotent activity for LRRK2 (G2019S) and wild-type LRRK2.
MK-1468 is >100-fold selective against 265 off-target kinases tested, and >1000-fold selectivity against a panel of 117 functional, enzyme, and radioligand binding assays screened (Cerep, Panlabs).
MK-1468 inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in the rat brain, orally active.
Physicochemical Properties
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M.Wt
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501.02
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Formula
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C26H33ClN4O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-N-(7-chloro-6-(4-((3R,4R)-4-hydroxy-3-methyltetrahydrofuran-3-yl)piperazin-1-yl)isoquinolin-3-yl)-6-oxaspiro[2.5]octane-1-carboxamide
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References
1. Kattar SD, et al. J Med Chem. 2023 Oct 20. doi: 10.1021/acs.jmedchem.3c01486.
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