| Bioactivity | LRRK2-IN-6 (compound 22) is a potent, orally active, selective leucine rich repeat protein kinase 2 gene (LRRK2) inhibitor with IC50 values of 4.6 and 49 μM for GS LRRK2 and WT LRRK2, respectively. LRRK2-IN-6 inhibits LRRK2 Ser1292 and Ser925 autophosphorylation. LRRK2-IN-6 can cross the blood-brain barrier[1]. |
| Target | IC50: 4.6 (GS LRRK2) and 49 μM (GS LRRK2) |
| Invitro | LRRK2-IN-6 (compound 22; 0-10000 nM; 24 h; HEK293 cells) has excellent potency and GS-LRRK2 selectivity[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | LRRK2-IN-6 (compound 22; 0.5 mg/kg (i.v.) and 5 mg/kg (p.o.); CD-1 mice) has good pharmacokinetic parametershigh and high bioavailability[1]. Animal Model: |
| Name | LRRK2-IN-6 |
| Formula | C23H24F2N4O2S |
| Molar Mass | 458.52 |
| 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]. Leśniak RK, et, al. Discovery of azaspirocyclic 1H-3,4,5-Trisubstitued pyrazoles as novel G2019S-LRRK2 selective kinase inhibitors. Eur J Med Chem. 2022 Nov 15;242:114693. |