438194
LRRK2 Inhibitor II, CZC-25146
The LRRK2 Inhibitor II, CZC-25146 controls the biological activity of LRRK2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
別名:
LRRK2 Inhibitor II, CZC-25146, N-(2-(5-Fluoro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl, N-(2-(2-(2-Methoxy-4-morpholinophenylamino)-5-fluoropyrimidin-4-ylamino)phenyl)methanesulfonamide, HCl
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この商品について
実験式（ヒル表記法）:
C22H25FN6O4S · xHCl
分子量:
488.54 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
gray to off-white
solubility
water: 1 mg/mL, DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
FC1=C(N=C(NC2=CC=C(N3CCOCC3)C=C2OC)N=C1)NC4=CC=CC=C4NS(=O)(C)=O.[xHCl]
General description
An orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50 = 4.76 and 6.87 nM for hr-wt-LRRK2 and G2019S-LRRK2 mutant, respectively) with selectivity over PLK4, GAK, TNK1, CAMKK2, and PIP4K2C (IC50<300 nM) in a 185-kinase panel. Does neither exert cytotoxicity nor block neuronal development of human or rat cortical neurons at 1 µM. Shown to prevent GS-LRRK2-induced neuronal injury (EC50 ~4 nM) and G2019S- or R1441C-LRRK2-mediated neuronal death in both rat and human cortical neurons (EC50 ~ 100 nM). Even though exhibits favorable pharmacokinetic profile and metabolic stability, and yet suffers from limited blood brain barrier penetration (~4%).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Ramsden, N., et al. 2011. ACS Chem. Biol.6, 1021.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable