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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₂₂H₂₅FN₆O₄S · xHCl
• Masa cząsteczkowa: 488.54 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder
• Quality level: 100
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Właściwości

• Quality Level: 100
• 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]

Opis

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)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable