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SBI-797812

    
10mM in DMSO

SBI-797812

源叶(MedMol)
T93691 一键复制产品信息
2237268-08-3
C19H22N4O4S
402.47
Urea,N-​[4-​(8-​oxa-​3-​azabicyclo[3.2.1]​oct-​3-​ylsulfonyl)​phenyl]​-​N'-​(4-​pyridinylmethyl)​-
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T93691-1ml促销
10mM in DMSO

¥720.00 ¥648.00

10 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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
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参考文献

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