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。
| 生物活性 | Crotedumab (REGN1193) is a fully humanIgG4monoclonal antibody that binds and inhibitsglucagon receptor(GCGR), with aKDof 0.1 nM. Crotedumab can be used for the research of diabetes[1][2]. |
| IC50& Target | |
体外研究
(In Vitro) | Crotedumab 以高亲和力 (KD=0.03 nM-0.39 nM) 结合来自多个物种 (小鼠、大鼠、猴子和人类) 的 GCGR[2]。
Crotedumab 通过 GCGR 抑制转染人、猴、小鼠和大鼠 GCGR 的 HEK293 细胞中胰高血糖素诱导的信号传导，IC50值分别为 0.65，3.2，0.94 和 1.0 nM[2 ]。
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体内研究
(In Vivo) | Crotedumab (3-30 mg/kg; 皮下注射，每周一次，持续 4 周) 可降低饮食引起的肥胖小鼠的血糖和体重，并诱导可逆性高胰高血糖素血症和 α 细胞增生[2]。
Crotedumab (10 mg/kg; 单次皮下注射) 持续 18 天显着降低糖尿病ob/ob小鼠的血糖[2]。
REGN1193 (20 mg/kg; 单次静脉注射) 可显着降低糖尿病食蟹猴意识和麻醉状态下的夜间空腹血糖以及进食后 1 小时测量的血糖[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. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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