crotedumab

Ligand id: 9614

Name: crotedumab

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

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
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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]