Bioactivity | LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability[1]. |
Invitro | LRRK2-IN-14 (1 μM; 30 min) 在肝微粒体中的代谢稳定性较高 (79.3%)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> LRRK2-IN-14 相关抗体: |
In Vivo | LRRK2-IN-14 (30 mg/kg; p.o.; single dose) 在 ICR 小鼠中抑制了大脑中 G2019S 突变的 LRRK2 的磷酸化[1]。在 ICR 小鼠中的药代动力学分析[1] Route |
CAS | 2942328-06-3 |
Formula | C17H18F3N5O2 |
Molar Mass | 381.35 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Kim K, et al. Concurrent Optimizations of Efficacy and Blood-Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson's Disease Therapeutics. J Med Chem. 2024 May 9;67(9):7647-7662. |