產品屬性：
產品名稱 | PFE-360 |
規格 | 10mM*1mL in DMSO、5mg、10mg、50mg、100mg、200mg、500mg |
貨號 | EY-01Y12865 |
Cas No.: 1527475-61-1
別名: N/A
化學名: N/A
分子式: C16H16N6O
分子量: 308.34
溶解度: DMSO: 10.42 mg/mL (33.79 mM)
儲存條件: 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
產品描述：
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.
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