CZC-25146 is a potent selective and metabolically stable inhibitor of leucine-rich repeat kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson’s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped that LRRK2 inhibitors may be useful in treating the disease. CZC-25146 was shown to prevent mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency.
| Molecular Weight | 525 |
| Formula | C22H25FN6O4S · HCl |
| CAS Number | 1330003-04-7 |
| Solubility (25°C) | DMSO: ≥15 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Related LRRK2 Products |
|---|
| PF-06371900
PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor. |
| PF-06455943
PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
