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PFE-360
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PFE-360图片
CAS NO:1527475-61-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
PFE-360 (PF-06685360) 是有效的、选择性的、能透过血脑屏障的、口服有效的 LRRK2 的抑制剂,体内测得的平均IC50 值为 2.3 nM。
Cas No.1527475-61-1
别名PF-06685360
Canonical SMILESN#CC1=CC(C2=CNC3=NC=NC(N4CCOCC4)=C32)=CN1C
分子式C16H16N6O
分子量308.34
溶解度DMSO: 10.42 mg/mL (33.79 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[1][2]. IC50: 2.3 nM (LRRK2 in vivo) [1][2].

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[1]. Animal Model: Female Sprague Dawley rats (NTac:SD) weighed 225-250 g[3].

[1]. Marco A.S. Baptista, et al. LRRK2 Kinase Inhibitors of Different Structural Classes Induce Abnormal Accumulation of Lamellar Bodies in Type II Pneumocytes in Non-Human Primates but are Reversible and Without Pulmonary Functional Consequences. [2]. Andersen MA, et al. Parkinson's disease-like burst firing activity in subthalamic nucleus induced by AAV-α-synuclein is normalized by LRRK2 modulation. Neurobiol Dis. 2018 Aug;116:13-27. [3]. Andersen MA, et al. PFE-360-induced LRRK2 inhibition induces reversible, non-adverse renal changes in rats. Toxicology. 2018 Feb 15;395:15-22.