PFE-360 (Synonyms: PF-06685360)
目录号: PL06796 纯度: ≥98%
CAS No. :1527475-61-1
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中文名称
PFE-360
英文名称
PFE-360
英文别名
PF-06685360;1-Methyl-4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1H-pyrrole-2-carbonitrile;BDBM185558;US9156845, 217;1-methyl-4-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)pyrrole-2-carbonitrile;PFE-360;AT26782
Cas No.
1527475-61-1
分子式
C16H16N6O
分子量
308.34
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
PFE-360 (PF-06685360) is a potent, selective, brain penetrated and orally active leucine-rich repeat kinase 2 (LRRK2) inhibitor with a mean IC 50 of 2.3 nM in vivo.
性状
Solid
IC50 & Target[1][2]
IC50: 2.3 nM (LRRK2 in vivo) .
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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. Parkinsons 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.
溶解度数据
In Vitro: DMSO : 10.42 mg/mL (33.79 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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