Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC₅₀s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively^[1].

NAMPT^[1]
CYP3A4^[1]

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 ^[1].
Nampt-IN-5 shows a good ADME data: mouse microsomal clearance (110 μl/min•mg), CYP3A4 inhibition value (0.75 μM), Sol_6.8: 0.056 mM; MDCK P_app AB: 18.6^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].
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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

427.50

C₂₅H₂₅N₅O₂

2380013-17-0

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (116.96 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.85 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.85 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.