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NF-56-EJ40 

Cat. No.: HY-130246
Handling Instructions

NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.

For research use only. We do not sell to patients.

NF-56-EJ40 Chemical Structure

NF-56-EJ40 Chemical Structure

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Description

NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM[1].

IC50 & Target

SUCNR1 (GPR91)[1]

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 Y832.64 and Y301.39 on one side, and R2817.39 on the other side. The conserved E181.27 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E221.31 and N2747.32 in human SUCNR1 are replaced by K181.31 and K2697.32 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 Y301.39F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E181.27K and E181.27R 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 K181.31E/K2697.32N (hereafter denoted humanized rat SUCNR1) (Ki 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[1].

Molecular Weight

443.54

Formula

C₂₇H₂₉N₃O₃

SMILES

O=C(NC1=C(CC(O)=O)C=CC=C1)C2=CC=CC(C3=CC=C(CN4CCN(C)CC4)C=C3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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KeyWords:

NF-56-EJ40 | Others | SUCNR1 | GPR91 | Inhibitor | inhibitor | inhibit

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NF-56-EJ40
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HY-130246
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