PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC50 of 2.3 nM in vivo.
IC50&Target
IC50: 2.3 nM (LRRK2 in vivo) .
体内研究
PFE-360 (4 mg/kg and 7.5 mg/kg, orally, BID, 10-12 weeks) treatment potently decreases the LRRK2-pSer935/total LRRK2 ratio, with no significant adverse effects.
Animal Model:
Female Sprague Dawley rats (NTac:SD) weighed 225-250 g.
Dosage:
4 mg/kg and 7.5 mg/kg (pharmacokinetics and pharmacodynamics).
Administration:
Orally BID for 10-12 weeks.
Result:
The LRRK2-pSer935/total LRRK2 ratio was significantly decreased at both 1 h and 12 h after dosing.
The terminal bodyweights exhibited no significant changes.
分子式
C16H16N6O
分子量
308.34
CAS号
1527475-61-1
运输条件
Room temperature in continental US; may vary elsewhere.