Nampt-IN-5
目录号: PL07694 纯度: ≥99%
CAS No. :2380013-17-0
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中文名称
Nampt-IN-5
英文名称
Nampt-IN-5
英文别名
Nampt-IN-5;N-[4-[(2-ethoxybenzimidazol-1-yl)methyl]phenyl]-3-pyridin-3-ylazetidine-1-carboxamide
Cas No.
2380013-17-0
分子式
C25H25N5O2
分子量
427.50
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Nampt-IN-5 是一种有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 抑制剂。Nampt-IN-5 还抑制 CYP3A4 活性。Nampt-IN-5 可抑制 A2780 和 COR-L23 细胞,IC50 值分别为 0.7 nM 和 3.9 nM。
生物活性
Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC 50 s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.
性状
Solid
IC50 & Target[1][2]
NAMPT
CYP3A4
体外研究(In Vitro)
Nampt-IN-5 (compound 27) (0-10 nM; 3 days) has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively .
Nampt-IN-5 shows a good ADME data: mouse microsomal clearance (110 μl/min?mg), CYP3A4 inhibition value (0.75 μM), Sol6.8: 0.056 mM; MDCK Papp AB: 18.6. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Nampt-IN-5 (5-30 mg/kg; p.o. twice daily for 4 days) causes a significant amount of body weight loss in nude mice relative to vehicle.
Nampt-IN-5 (10 mg/kg; p.o.) exhibits T 1/2 (2.1 h), C max (29112 nM), and AUC (61984 nM?h) in mice. 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;In solvent -80°C 6 months
参考文献
[1]. Palacios DS, et al. Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).ACS Med Chem Lett. 2019 Oct 10;10(11):1524-1529.
溶解度数据
In Vitro: DMSO : 50 mg/mL (116.96 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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