| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S422688-1ml |
1ml |
现货  |
|
| 英文别名 | Urea,N-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-ylsulfonyl)phenyl]-N'-(4-pyridinylmethyl)- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | SBI-797812 |
| 生化机理 | SBI-797812 是一种 NAMPT 激活剂，在结构上与活性位点定向 NAMPT 抑制剂相似，并能阻断这些抑制剂与 NAMPT 的结合。SBI-797812 可将 NAMPT 转化为 "超级催化剂"，从而更有效地生成 NMN。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
SBI-797812 是一种口服有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 激活剂。SBI-797812 激活 NAMPT 向 NMN 转变，增加 NAMPT 对 ATP 的亲和力，稳定磷酸化 NAMPT，促进焦磷酸盐副产物的消耗，并减弱 NAD+ 的反馈抑制。SBI-797812 增加细胞内 NMN，并提高小鼠肝脏内 NAD+ 水平。 Information SBI-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. Targets NAMPT In vitro SBI-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 vivo Plasma 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 |
| ALogP | 0.702 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 5 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 未知 |
|---|---|
| IIUPAC Name | 1-[4-(8-oxa-3-azabicyclo[3.2.1]octan-3-ylsulfonyl)phenyl]-3-(pyridin-4-ylmethyl)urea |
| INCHI | 1S/C19H22N4O4S/c24-19(21-11-14-7-9-20-10-8-14)22-15-1-5-18(6-2-15)28(25,26)23-12-16-3-4-17(13-23)27-16/h1-2,5-10,16-17H,3-4,11-13H2,(H2,21,22,24) |
| InChi Key | KTSOHNHLOLGQCY-UHFFFAOYSA-N |
| Smiles | C1CC2CN(CC1O2)S(=O)(=O)C3=CC=C(C=C3)NC(=O)NCC4=CC=NC=C4 |
| Isomeric SMILES | C1CC2CN(CC1O2)S(=O)(=O)C3=CC=C(C=C3)NC(=O)NCC4=CC=NC=C4 |
| PubChem CID | 135222620 |
| 分子量 | 402.47 |
| DMSO(mg / mL) Max Solubility | 80 |
|---|---|
| DMSO(mM) Max Solubility | 198.772579322682 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 402.500 g/mol |
| XLogP3 | 0.700 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 6 |
| 可旋转键计数Rotatable Bond Count | 5 |
| 精确质量Exact Mass | 402.136 Da |
| 单同位素质量Monoisotopic Mass | 402.136 Da |
| 拓扑极表面积Topological Polar Surface Area | 109.000 Ų |
| 重原子数Heavy Atom Count | 28 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 627.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 2 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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