maridebart cafraglutide   Click here for help

GtoPdb Ligand ID: 13316

Synonyms: AMG 133 [3] | AMG-133 | AMG133 | MariTide
Compound class: Antibody
Comment: Maridebart cafraglutide (AMG133) is an anti-human gastric inhibitory polypeptide receptor (GIPR) antagonist antibody-peptide conjugate [1,3]. It has two attached glucagon-like peptide 1 (GLP-1) agonist peptides (cafraglutide). Maridebart cafraglutide is proposed to ellicit synergistic effects (antagonism of GIPR signalling and activation of GLP-1 receptor signalling) to regulate body weight for application as an anti-obesity modality [2-3].
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Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
GLP-1 receptor Rn Agonist Agonist 8.6 pEC50 - 3
pEC50 8.6 (EC50 2.4x10-9 M) [3]
Description: In vitro potency in GLP-1R recombinant cells
GLP-1 receptor Monkey Agonist Agonist 8.2 pEC50 - 3
pEC50 8.2 (EC50 5.7x10-9 M) [3]
Description: In vitro potency in GLP-1R recombinant cells
GLP-1 receptor Hs Agonist Agonist 7.6 pEC50 - 3
pEC50 7.6 (EC50 2.44x10-8 M) [3]
Description: In vitro potency in GLP-1R recombinant cells
GIP receptor Monkey Antagonist Antagonist 7.6 pIC50 - 3
pIC50 7.6 (IC50 2.65x10-8 M) [3]
Description: In vitro potency in GIPR recombinant cells
GIP receptor Hs Antagonist Antagonist 7.4 pIC50 - 3
pIC50 7.4 (IC50 4.24x10-8 M) [3]
Description: In vitro potency in GIPR recombinant cells
GIP receptor Rn Antagonist Antagonist 6.1 pIC50 - 3
pIC50 6.1 (IC50 8.223x10-7 M) [3]
Description: In vitro potency in GIPR recombinant cells