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Mazdutide

(Synonyms: IBI-362; LY-3305677; OXM-3) 目录号 : GC69439 复制 一键复制产品信息

Mazdutide是一种有长效作用的胰高血糖素样肽-1受体(GLP-1R;Ki=28.6nM)和胰高血糖素受体(GCGR;Ki=17.7nM)双重激动剂。

Mazdutide Chemical Structure

Cas No.:2259884-03-0

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1mg
¥880.00
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5mg
¥2,640.00
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10mg
¥4,400.00
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Sample solution is provided at 25 µL, 10mM.

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Description

Mazdutide is a long-acting dual agonist of the glucagon-like peptide-1 receptor (GLP-1R; Ki=28.6nM) and the glucagon receptor (GCGR; Ki=17.7nM)[1-2]. Mazdutide can suppress appetite and slow gastric emptying by activating the GLP-1 receptor to reduce energy intake, while simultaneously increasing energy expenditure and promoting hepatic fat breakdown by activating the GCG receptor to improve metabolism. Mazdutide is used for the long-term management of adult overweight/obesity and the treatment of type 2 diabetes[3-4].

In vivo, db/db mice were subcutaneously administered Mazdutide (50-200μg/kg) once every three days for 12 consecutive weeks. Mazdutide significantly improved diabetes-associated cognitive dysfunction[5]. C57BL/6J male mice with obesity induced by a 13-week high-fat diet were subcutaneously administered Mazdutide (15nmol/kg) once every three days for 4 weeks. Mazdutide significantly reduced hepatic fat accumulation, and its effect was superior to that of a GLP-1R mono-agonist[6].

References:
[1] Shirley M. Mazdutide: First Approval. Drugs. 2025 Dec;85(12):1621-1627.
[2] Pan XF, Fang ZZ, Zhang L, et al. Obesity in China: current progress and future prospects. Lancet Diabetes Endocrinol. 2026 Feb;14(2):178-186.
[3] Bailey CJ, Flatt PR, Conlon JM. Multifunctional incretin peptides in therapies for type 2 diabetes, obesity and associated co-morbidities. Peptides. 2025 May;187:171380.
[4] Sidrak WR, Kalra S, Kalhan A. Approved and Emerging Hormone-Based Anti-Obesity Medications: A Review Article. Indian J Endocrinol Metab. 2024 Sep-Oct;28(5):445-460.
[5] Dong W, Bai J, Yuan Q, Z, et al. Mazdutide, a dual agonist targeting GLP-1R and GCGR, mitigates diabetes-associated cognitive dysfunction: mechanistic insights from multi-omics analysis. EBioMedicine. 2025 Jul;117:105791.
[6] Xia H, Min Y, Wang Y, et al. Multiparametric MRI Evaluation of Liver Fat and Iron after Glucagon-like Peptide-1 Receptor and Glucagon Receptor Dual-Agonist Treatment in a High-Fat Diet-induced Mouse Model. Radiology. 2025 Aug;316(2):e243780.

Mazdutide是一种有长效作用的胰高血糖素样肽-1受体(GLP-1R;Ki=28.6nM)和胰高血糖素受体(GCGR;Ki=17.7nM)双重激动剂[1-2]。Mazdutide可通过激活GLP-1受体抑制食欲、延缓胃排空以减少能量摄入,同时通过激活GCG受体增加能量消耗、促进肝脏脂肪分解以改善代谢。Mazdutide可用于成人超重/肥胖的长期体重管理和2型糖尿病的治疗[3-4]

在体内,Mazdutide(50-200μg/kg)每三天一次皮下注射,用于处理的db/db小鼠,连续12周。Mazdutide显著改善了糖尿病相关的认知功能障碍[5]。Mazdutide(15nmol/kg)每三天一次皮下注射,用于处理经13周高脂饮食诱导的C57BL/6J雄性肥胖小鼠,持续4周。Mazdutide显著减少了肝脏脂肪积累,且效果优于GLP-1R单激动剂[6]

实验参考方法

Animal experiment [1]:

Animal models

db/db mice

Preparation Method

Male db/db mice were subcutaneously administered three escalating doses of Mazdutide (50, 100, 200μg/kg) or dulaglutide (200μg/kg) once every three days for 12 weeks. Cognitive function, metabolic parameters, brain pathology, and molecular pathways were evaluated at the end of treatment.

Dosage form

50, 100, 200μg/kg; s.c.; Once every three days for 12 weeks.

Applications

Mazdutide administration led to significant body weight loss, improved glycemic control, and ameliorated diabetes-associated cognitive dysfunction. Mazdutide improved performance in behavioral tests, reduced neuronal injury and myelin decline in the hippocampus, and modulated pathways related to neurotransmission, neuroinflammation, and synaptic plasticity.

References:
[1] Dong W, Bai J, Yuan Q, Z, et al. Mazdutide, a dual agonist targeting GLP-1R and GCGR, mitigates diabetes-associated cognitive dysfunction: mechanistic insights from multi-omics analysis. EBioMedicine. 2025 Jul;117:105791.

化学性质

Cas No. 2259884-03-0 SDF Download SDF
别名 IBI-362; LY-3305677; OXM-3
分子式 分子量 4563.06
溶解度 H2O : 22.22 mg/mL (ultrasonic and adjust pH to 2 with HCl) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 219.2 μL 1.0958 mL 2.1915 mL
5 mM 43.8 μL 219.2 μL 438.3 μL
10 mM 21.9 μL 109.6 μL 219.2 μL
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