LRRK2 Inhibitor II; CZC-25146

Code: 438194-10MG D2-231

General description

An orally bioavailable fluoro-diaminopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of LRRK2 activity (IC50

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Your Price
€227.74 10MG
€280.12 inc. VAT

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%).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ramsden, N., et al. 2011. ACS Chem. Biol.6, 1021.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)

assay≥98% (HPLC)
colorgray to off-white
formpowder
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
SMILES stringFC1=C(N=C(NC2=CC=C(N3CCOCC3)C=C2OC)N=C1)NC4=CC=CC=C4NS(=O)(C)=O.[xHCl]
solubilityDMSO: 5 mg/mL, water: 1 mg/mL
storage conditiondesiccated (hygroscopic), protect from light, OK to freeze
storage temp.2-8°C
Cas Number1330003-04-7
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