PFE-360

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PFE-360 是一种新型有效、选择性、脑穿透性 LRRK2 抑制剂，IC50 为 3 nM。

PFE-360 is a novel potent, selective, brain-penetrating LRRK2 inhibitor with IC50 of 3 nM; induces a morphological kidney phenotype resembling that of the LRRK2 ko rats, whereas no effects in the lung; PFE-360 treatment induces morphological changes characterised by darkened kidneys and progressive accumulation of hyaline droplets in the renal proximal tubular epithelium, the estimated PFE-360 unbound plasma concentration off 10-fold the IC50 (30 nM) to achieve full peripheral LRRK2 inhibition.

——

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.

PFE360

Autophagy

LRRK2

LRRK2

——

——

1527475-61-1

308.345

C16H16N6O

>98% (HPLC)

DMSO : 10.42 mg/mL 33.79 mM

N#CC1=CC(C2=CNC3=NC=NC(N4CCOCC4)=C32)=CN1C

1-methyl-4-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)pyrrole-2-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years