货号	规格	价格	上海	北京	珠海	重庆	武汉
S81358-5mg买3赠1	99.48%	￥360.00 S81358-5mg ￥360.00 现货（买3赠1）	5 5	-	-	-	-
S81358-10mg买3赠1	99.48%	￥560.00 S81358-10mg ￥560.00 现货（买3赠1）	19 >10	-	-	-	-
S81358-25mg买3赠1	99.48%	￥1120.00 S81358-25mg ￥1120.00 现货（买3赠1）	4 4	-	-	-	-
S81358-50mg买3赠1	99.48%	￥1840.00 S81358-50mg ￥1840.00 现货（买3赠1）	1 0 1	-	-	-	-
S81358-100mg买3赠1	99.48%	￥2400.00 S81358-100mg ￥2400.00 现货（买3赠1）	6 6	-	-	-	-
S81358-200mg买3赠1	≥99%	￥4110.00 S81358-200mg ￥4110.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.

靶点：

IC50: 3 nM (LRRK2);LRRK2

体外研究：

PF-06447475 inhibits LRRK2 enzyme and LRRK2 in the whole cell assay with IC50s of 3 and 25 nM, respectively. Cells incubated with PF-06447475 alone (0.5, 1, 3 μM) or in the presence of ROT significantly reduces (S935)-LRRK2 kinase phosphorylation to control. PF-06447475 significantly preserves the nucleus morphology and ΔΨm of NLCs exposed to ROT compared to untreated and control. PF-475 significantly diminishes ROT-induced ROS generation to a similar extent to cells exposed to PF-475 alone

体内研究：

In G2019S+ rats treated with PF-06447475, a significant reduction in microgliosis to levels found in wild-type rats could be observed. The proinflammatory marker MHC-II expressed on myeloid cells but not neurons also appears to be less abundant in confocal sections in G2019S+ rats treated with PF-06447475. PF-06447475 treatment in G2019S+ rats significantly lowers the number of CD68 cells recruited to the SNpc. PF-06447475 successfully blocks the enhanced neuroinflammation associated with G2019S-LRRK2 expression. Treatment of G2019S+ rats with PF-06447475 preserves TH expression in the dorsal striatum, consistent with drug attenuating neurodegeneration in the SNpc. PF-06447475 is well tolerated in rats

参考文献：

1. Henderson JL, et al. Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor. J Med Chem. 2015 Jan 8;58(1):419-32. 2. Mendivil-Perez M, et al. Neuroprotective Effect of the LRRK2 Kinase Inhibitor PF-06447475 in Human Nerve-Like Differentiated Cells Exposed to Oxidative Stress Stimuli: Implications for Parkinson's Disease. Neurochem Res. 2016 Oct;41(10):2675-2692. 3. Daher JP, et al. Leucine-rich Repeat Kinase 2 (LRRK2) Pharmacological Inhibition Abates α-Synuclein Gene-induced Neurodegeneration. J Biol Chem. 2015 Aug 7;290(32):19433-44.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.275 ml	16.376 ml	32.751 ml
5 mM	0.655 ml	3.275 ml	6.55 ml
10 mM	0.328 ml	1.638 ml	3.275 ml
50 mM	0.066 ml	0.328 ml	0.655 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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