Crotedumab  (Synonyms: 克罗特度单抗; REGN1193; Anti-GCGR Reference Antibody (crotedumab))

Crotedumab (REGN1193) is a fully human IgG4 monoclonal antibody that binds and inhibits glucagon receptor (GCGR), with a K_D of 0.1 nM. Crotedumab can be used for the research of diabetes^[1][2].

Human IgG4 kappa

Human IgG4 (S228P) kappa, Isotype Control

Human

KD: 0.1 nM^[2]

Crotedumab 以高亲和力 (K_D=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 ]}。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1452387-69-7

液体

Colorless to light yellow

克罗特度单抗

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG4 kappa

• 
  Immobilized GCGR Protein, Human can bind Crotedumab. The EC₅₀ for this effect is 32.62 ng/mL.

• [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.  [Content Brief]

  [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.  [Content Brief]