PFE-360 (Synonyms: PF-06685360) |
| رقم الكتالوجGC36888 |
PFE-360 (PF-06685360) هو مثبط قوي ، انتقائي ، مخترق في الدماغ ونشط عن طريق الفم غني بالليوسين المتكرر كيناز 2 (LRRK2) مع متوسط IC50 من 2.3 نانومتر في الجسم الحي
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Cas No.: 1527475-61-1
Sample solution is provided at 25 µL, 10mM.
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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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