Crotedumab
Crotedumab Basic information
- Product Name:
- Crotedumab
- Synonyms:
-
- Crotedumab
- Research Grade Crotedumab(DHE51802)
- REGN1193
- Research Grade Crotedumab
- Crotedumab (anti-GCGR)
- CAS:
- 1452387-69-7
- MW:
- 0
- Mol File:
- Mol File
Crotedumab Chemical Properties
- form
- Liquid
- color
- Colorless to light yellow
Crotedumab Usage And Synthesis
Uses
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].
in vivo
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].
| Animal Model: | Diet-induced obese (DIO) male C57BL/6NTac mice were maintained on high-fat diet[2] |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | S.c. injection once weekly for 4 weeks |
| Result: | Markedly reduced blood glucose throughout the dosing period. Reversibly decreased body weight during the dosing period. Dose- and time-dependently increased glucagon and GLP-1. Reversibly increased α-cell area. |
References
[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. DOI:10.1111/dom.13075
[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. DOI:10.1210/en.2015-1011
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