NF-56-EJ40 is a potent, high-affinity, and highly selectivehuman SUCNR1 (GPR91)antagonist with anIC₅₀of 25 nM and aK_iof 33 nM, and shows almost no activity towards ratSUCNR1. NF-56-EJ40 has high affinity forhumanized rat SUCNR1with aK_ivalue of 17.4 nM^[1].

SUCNR1 (GPR91)^[1]

NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y83^2.64and Y30^1.39on one side, and R281^7.39on the other side. The conserved E18^1.27is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E22^1.31and N274^7.32in human SUCNR1 are replaced by K181.31 and K269^7.32in 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^[1].
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_iof 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^[1].

443.54

Solid

C₂₇H₂₉N₃O₃

2380230-73-7

Room temperature in continental US; may vary elsewhere.

DMSO : 5 mg/mL(11.27 mM;Need ultrasonic)

H₂O : 4.55 mg/mL(10.26 mM;ultrasonic and adjust pH to 9 with NaOH)

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