human GIP(3-42)NH2   Click here for help

GtoPdb Ligand ID: 8970

Comment: GIP(3-42)NH2 is a truncated form of gastric inhibitory polypeptide (GIP) formed through degradation by dipeptidyl peptidase IV (DPP IV). At high concentration GIP(3-42)NH2 acts as a low potency antagonist of the GIP receptor, weakly antagonizing cAMP accumulation and insulin output in vitro, but no physiological antagonism is observed in vivo [1].
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Bioactivity Comments
GIP(3-42) binds the human GIP receptor with an IC50 value of 22 nM, but does not activate receptor-mediated signalling [1].
Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
GIP receptor Hs Antagonist Binding 7.7 pIC50 - 1
pIC50 7.7 (IC50 2.2x10-8 M) [1]
Description: Binding affinity for the human receptor expressed in COS7 cells.
GIP receptor Hs Antagonist Antagonist 6.1 – 7.0 pIC50 - 1
pIC50 6.1 – 7.0 (IC50 7.31x10-7 – 9.2x10-8 M) [1]
Description: Measuring in vitro inhibition of native GIP-induced cAMP accumulation at [GIP] of 10 pM and 1 nM.