计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
NF-56-EJ40
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC 50 of 25 nM and a K i of 33 nM, and shows almost no activity towards rat SUCNR1 . NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a K i value of 17.4 nM
In Vitro
NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y83 2.64 and Y30 1.39 on one side, and R281 7.39 on the other side. The conserved E18 1.27 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E22 1.31 and N274 7.32 in human SUCNR1 are replaced by K181.31 and K269 7.32 in rat SUCNR1. These two amino acid exchanges could prevent the binding of NF-56-EJ40 to rat SUCNR1 owing to steric hindrance. Radioligand-binding studies with human SUCNR1 showed partial agreement with our homology model: the Y30 1.39 F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E18 1.27 K and E18 1.27 R mutants, probably owing to steric clashes of the Lys and Arg residues with NF-56-EJ40 and the loss of a hydrogen bond to its piperazine ring. Human SUCNR1 residues are introduced into rat SUCNR1 to form the double mutant K18 1.31 E/K269 7.32 N (hereafter denoted humanized rat SUCNR1) ( K i of 17.4 nM and 33.5 nM for human and humanized rat SUCNR1, respectively). NF-56-EJ40 increases the thermal stability of both humanized rat SUCNR1 and human SUCNR1, but not that of rat SUCNR1. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:SUCNR1 (GPR91)
规格
规格或纯度
Moligand™,10mM in DMSO
英文名称
NF-56-EJ40
生化机理
NF-56-EJ40 是一种强效、高亲和力和高选择性的人 SUCNR1（GPR91）拮抗剂，IC 50 为 25 nM，K i 为 33 nM，对大鼠 SUCNR1 几乎没有活性。NF-56-EJ40 与人源化大鼠 SUCNR1 具有很高的亲和力，其 K i 值为
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CCN(CC1)CC2=CC=C(C=C2)C3=CC(=CC=C3)C(=O)NC4=CC=CC=C4CC(=O)O
PubChem CID
分子量
443.54
技术文档
高级数据
关联靶点（人）
SUCNR1
Tchem
琥珀酸受体 1(Succinate receptor 1)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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