KKL 顾客使用本产品发表的 2 篇科研文献

NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC₅₀ 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.

NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y83 and Y30 on one side, and R281 on the other side. The conserved E18 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E22 and N274 in human SUCNR1 are replaced by K181.31 and K269 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 Y30F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E18K and E18R 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 K18E/K269N (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.

Room temperature in continental US; may vary elsewhere.

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