VPAC1 Receptor Antagonist
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Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27)
0 ImagesAcetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) is a high-affinity, selective VPAC1 receptor antagonist, with IC50 values of 10 nM and 2000 nM for binding to human VPAC1 and VPAC2, respectively. Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) inhibits VIP-induced VPAC1/Gs/adenylate cyclase signaling with a Ki of 2 nM, and its VPAC1 selectivity is mainly determined by the N-terminal extracellular domain of the receptor. Acetyl-(D-Phe2,Lys15,Arg16,Leu27)-VIP (1-7)-GRF (8-27) can be used in studies related to VPAC1 receptor pharmacology, VIP signaling, and the structure and function of class B GPCRs.
