| 产品描述: | NAMPT 活化剂;NAMPT Activators;;InformationSBI-797812 SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT . SBI-797812 turns NAMPT into a "super catalyst" that more efficiently generates NMN.TargetsNAMPTIn vitroSBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+.In vivoPlasma concentrations of SBI-797812 after oral administration are low. Higher plasma levels of SBI-797812 are seen after i.p. dosing. The potency of SBI-797812 against mouse NAMPT is investigated. The apparent affinity (EC50) of SBI-797812 for mouse NAMPT is approximately 8-fold less than for human NAMPT, whereas maximal fold activation by SBI-797812 is comparable between the mouse and human NAMPT. Dosing of mice with SBI-797812 elevates liver NAD+.Cell Research(from reference)Cell lines:Human A549 lung carcinoma cells Concentrations:10 μM Incubation Time:4 h |
| 靶点: |
NAMPT |
| 体内研究: |
SBI-797812 (10 mg/kg;ip 或 op;单剂量) 通过腹膜内注射显示高血浆暴露,Cmax 值为 3297 ng/mL,8.2 μM。 SBI-797812 (20 mg/kg;腹腔注射;单剂量;给药后 2 小时测量) 显著增加小鼠肝脏中的 NAD+。 |
| 参考文献: |
1. Gardell SJ , et al. Boosting NAD+ with a small molecule that activates NAMPT. Nat Commun. 2019 Jul 19;10(1):3241. 2. Khaidizar FD, et al. Nicotinamide Phosphoribosyltransferase as a Key Molecule of the Aging/Senescence Process. Int J Mol Sci. 2021 Apr 2;22(7):3709. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.485 ml |
12.423 ml |
24.847 ml |
| 5 mM |
0.497 ml |
2.485 ml |
4.969 ml |
| 10 mM |
0.248 ml |
1.242 ml |
2.485 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.497 ml |
|
| 注意: |
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