NNC-0640 is an effective negative allosteric modulator (NAM) of the human glucagon receptor (GCGR), with an IC50 value of 69.2 nM. NNC-0640 binds to the external surface of the GCGR transmembrane domain, forms hydrogen bonds with residues S350, T353, and N404, and makes hydrophobic contacts with helices VI and VII. NNC-0640 stabilizes inactive GCGR conformation via a compact stalk and ECL1 beta-sheet structure that caps the orthosteric ligand-binding pocket. NNC-0640 can be used for the researches of type 2 diabetes[1][2].
Molecular Weight:
573.67
Purity:
98.43
CAS Number:
[307986-98-7]
Formula:
C29H31N7O4S
Target:
GCGR
Application Notes:
MCE Product type: Reference compound
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