Crotedumab

• CAT Number: I042235
• CAS Number: 1452387-69-7
• Purity: ≥95%

Crotedumab (REGN1193) is a fully human IgG4 monoclonal antibody that binds and inhibits glucagon receptor (GCGR), with a KD of 0.1 nM. Crotedumab can be used for the research of diabetes[1][2].
Crotedumab binds to GCGR from multiple species (mouse, rat, monkey, and humans) with high affinity (KD=0.03 nM-0.39 nM)[2].
Crotedumab inhibits Glucagon-induced signaling through GCGR with IC50s of 0.65, 3.2, 0.94 and 1.0 nM in HEK293 cells transfected with GCGR from human, monkey, mouse, and rat, respectively[2].
Crotedumab (3-30 mg/kg; s.c. once weekly for 4 weeks) reduces blood glucose and body weight and induces reversible hyperglucagonemia and α-cell hyperplasia in DIO C57BL/6 mice[2].
Crotedumab (10 mg/kg; a single s.c.) markedly decreases blood glucose for 18 days in diabetic ob/ob mice[2].
REGN1193 (20 mg/kg; a single i.v.) produces a robust reduction in overnight-fasted blood glucose in both the conscious and anesthetized state of diabetic cynomolgus monkeys as well as in blood glucose measured 1 hour after feeding[2].

Reference

[1]. Kostic A, et, al. A first-in-human pharmacodynamic and pharmacokinetic study of a fully human anti-glucagon receptor monoclonal antibody in normal healthy volunteers. Diabetes Obes Metab. 2018 Feb;20(2):283-291.
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[2]. Okamot H, et, al. Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys. Endocrinology. 2015 Aug;156(8):2781-94.
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