PF-06260933
目录号: PL06945 纯度: ≥99%
CAS No. :1811510-56-1
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中文名称
PF-06260933
英文名称
PF-06260933
英文别名
PF-06260933;5-(4-Chlorophenyl)-[3,3']bipyridinyl-6,6'-diamine;5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine;TQR1219;BCP28968;BDBM50134771;s6499;PF6260933;PF06260933; PF 06260933;5-(6-aminopyridin-3-yl)-3-(4-chlorophenyl)pyridin-2-amine
Cas No.
1811510-56-1
分子式
C16H13ClN4
分子量
296.75
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PF-06260933 是一种具有口服活性的,高度选择性的 MAP4K4 小分子抑制剂,在激酶实验和细胞实验中的 IC50 值分别为 3.7 和 160 nM。
生物活性
PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC 50 s of 3.7 and 160 nM for kinase and cell, respectively.
性状
Solid
IC50 & Target[1][2]
MAP4K4 3.7 nM (IC50)
体外研究(In Vitro)
PF-06260933 treatment of human aortic endothelial cell (EC) robustly prevents TNF-α-mediated endothelial permeability in vitro , similar to MAP4K4 knockdown. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In the mice model, PF-06260933 treatment does not alter plasma lipid content, although reductions in glucose levels are observed, which is consistent with whole-body-inducible Map4k4 knockout animals. PF-06260933 administration ameliorates further plaque development and/or promotes plaque regression in this animal model (46.0% versus 25.5%), and a reduction in plasma glucose as well as lipid content is also observed. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33.
[2]. Roth Flach RJ, et al. Endothelial protein kinase MAP4K4 promotes vascular inflammation and atherosclerosis. Nat Commun. 2015 Dec 21;6:8995.
溶解度数据
In Vitro: DMSO : 30 mg/mL (101.10 mM; Need ultrasonic and warming)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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