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CAS No. : 1452387-69-7
MCE 国际站:Crotedumab
产品活性:Crotedumab (REGN1193) 是一种人源化的 IgG4 单克隆抗体,可结合并抑制胰高血糖素受体 (GCGR),KD 值为 0.1 nM。Crotedumab 可用于糖尿病的研究。
研究领域:GPCR/G Protein
作用靶点:GCGR
In Vitro: Crotedumab binds to GCGR from multiple species (mouse, rat, monkey, and humans) with high affinity (KD=0.03 nM-0.39 nM).
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.
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.
Crotedumab (10 mg/kg; a single s.c.) markedly decreases blood glucose for 18 days in diabetic ob/ob mice.
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.
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