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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-NAMPT-SBI-797812
SBI-797812

Chemical Structure : SBI-797812

CAS No.: 2237268-08-3

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SBI-797812 (SBI 797812)

货号: PC-73039Not For Human Use, Lab Use Only.

SBI-797812 (SBI 797812) is a specific small molecule NAMPT activator with EC50 of 0.37 uM, increases NAMPT-catalyzed NMN synthesis by 2.1-fold (Emax).

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SBI-797812 (SBI 797812) is a specific small molecule NAMPT activator with EC50 of 0.37 uM, increases NAMPT-catalyzed NMN synthesis by 2.1-fold (Emax).
SBI-797812caused concentration-dependent activation of human NAMPT-mediated NMN production in the presence of NAM, PRPP and ATP, activating NAMPT via SBI-797812 was abolished by NAMPT inhibitors including GNI-50, FK-866, and CHS-828.
SBI-797812 also binds to the NAMPT active site, The Km values of NAMPT for ATP without and with SBI-797812 were 1.73 ± 0.32 and 0.29 ± 0.03 mM, respectively.
SBI-797812 impacted PP consumption and pHisNAMPT reactivity.
SBI-797812 dose-dependently elevated of intracellular NMN and NAD+ levels in A549 cells with 1.5, 1.7, and 2.2-fold in the presence of 0.4, 2, and 10 uM SBI-797812.
SBI-797812 promoted PARP-1 activity in the cellular lysate.
SBI-797812 (20 mg kg−1 i.p.) caused a significant 1.3-fold increase of NAD+ was detected in liver and cardiac tissue in treated mice.

物理化学性质&存储条件

分子量 402.469
分子式 C19H22N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(4-(((1R,5S)-8-Oxa-3-azabicyclo[3.2.1]octan-3-yl)sulfonyl)phenyl)-3-(pyridin-4-ylmethyl)urea

参考文献

1. Gardell SJ, et al. Nat Commun. 2019 Jul 19;10(1):3241.

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