GtoPdb Ligand ID: 9614

Synonyms: REGN-1193 | REGN1193
Compound class: Antibody
Comment: Crotedumab (REGN1193) is a fully human IgG4 monoclonal antibody that functionally antagonises activity of the glucagon receptor (GCGR) in vitro [1]. REGN1193 was investigated as a potential therapy for type 2 diabetes mellitus.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
This mAb is no longer included in Regeneron's development pipeline (access their pipeline webpage here).
Bioactivity Comments
REGN1193 cross-reacts with mouse, rat, monkey, and human GCGRs, which facilitates effective preclinical assessment of efficacy and safety [1]. REGN1193 inhibits glucagon-induced hGCGR signalling (cAMP) with an IC50 of 0.65 nM in a cell-based luciferase reporter system [1]. The antibody reduces blood glucose levels in diabetic ob/ob mice.
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
glucagon receptor Rn Antibody Antagonist 10.8 pKd - 1
pKd 10.8 (Kd 1.5x10-11 M) [1]
glucagon receptor Mm Antibody Antagonist 10.1 – 10.5 pKd - 1
pKd 10.1 – 10.5 (Kd 8.99x10-11 – 3.05x10-11 M) [1]
glucagon receptor Monkey Antibody Antagonist 9.4 – 10.5 pKd - 1
pKd 9.4 – 10.5 (Kd 3.86x10-10 – 3.03x10-11 M) [1]
glucagon receptor Hs Antibody Antagonist 9.8 – 10.0 pKd - 1
pKd 9.8 – 10.0 (Kd 1.62x10-10 – 1.09x10-10 M) [1]