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NF-56-EJ40

CAS No. : 2380230-73-7

MCE 站：NF-56-EJ40

产品活性：NF-56-EJ40 是一种有效，高亲和力和高度选择性的人 SUCNR1 (GPR91) 拮抗剂，IC₅₀ 为 25 nM，K_i 为 33.5 nM，对大鼠 SUCNR1 几乎没有活性。 NF-56-EJ40 对人源化大鼠 SUCNR1 具有高亲和力，K_i 值为 17.4 nM。

研究领域：Others

作用靶点：Others

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 Y30^1.39F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E18^1.27K and E18^1.27R 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 K18^1.31E/K269^7.32N (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.

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