Bioactivity | (R,R)-LRRK2-IN-7 is the isomer of LRRK2-IN-7 (HY-152107). LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase?inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1]. |
Target | IC50: 0.9 nM (LRRK2 Kinase) |
Invitro | LRRK2-IN-7 (compound 25) 既是小鼠乳腺癌抗性蛋白 (BCRP) 底物(小鼠/人 BCRP)也是一种有效的人 BCRP 抑制剂(BCRP IC50 = 0.12 μM)[1] . |
In Vivo | 在一项为期 7 天的大鼠剂量限制毒性研究中,LRRK2-IN-7 (compound 25) 的耐受性高达 100 mg/kg,每天一次(AUCtot = 330 μM·h)[1]。在大鼠急性(2 小时)PK/PD 研究中,LRRK2-IN-7 (compound 25) 显示大鼠脑纹状体中 LRRK2 pS935 剂量依赖性降低,EC50 = 0.18 nM[1]。 |
Name | (R,R)-LRRK2-IN-7 |
CAS | 2307277-92-3 |
Formula | C24H26N6O |
Molar Mass | 414.50 |
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]. David A Candito, et al. Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1 H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease. J Med Chem. 2022 Dec 22;65(24):16801-16817. |