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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-Cotadutide
Cotadutide

Chemical Structure : Cotadutide

CAS No.: 1686108-82-6

Cotadutide (MEDI-0382, MEDI0382)

货号: PC-72605Not For Human Use, Lab Use Only.

Cotadutide (MEDI-0382, MEDI0382) is a potent dual GLP-1/glucagon receptor peptide agonist with EC50 values of 6.9 pM and 10.2 pM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cotadutide (MEDI-0382, MEDI0382) is a potent dual GLP-1/glucagon receptor peptide agonist with EC50 values of 6.9 pM and 10.2 pM, respectively.
Cotadutide (MEDI-0382, MEDI0382) stimulates a concentration-dependent increase in cAMP accumulation in rat (INS-1 832/3) and human (EndoC-βH1) β-cell lines (EC50: 226 pM and 1051 pM, respectively ), as well as rat, mouse and human hepatocytes (EC50: 462 pM, 840 pM, 1447 pM, respectively).
Cotadutide (MEDI-0382, MEDI0382) potentiates glucose-stimulated insulin secretion in the rat (INS-1 832/3) pancreatic β‐cell line and increases glucose output in rat hepatocytes.
Cotadutide (MEDI-0382, MEDI0382) induces mitochondrial turnover and enhances mitochondrial function in mouse primary hepatocytes.
Cotadutide (MEDI-0382, MEDI0382) (10- 30 nmol/kg, s.c.) suppresses food intake and reduces body weight in DIO mice, reduces hepatic fibrosis and inflammation in in ob/ob AMLN NASH mice.

物理化学性质&存储条件

分子量 3728.0
分子式 C167H252N42O55
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (37.3 mg/mL)

Chemical Name/SMILES

H-His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Lys(1)-Ser-Glu-Tyr-Leu-Asp-Ser-Glu-Arg-Ala-Arg-Asp-Phe-Val-Ala-Trp-Leu-Glu-Ala-Gly-Gly-OH.palmitoyl-Glu(1)-OH

参考文献

1. Henderson SJ, et al. Diabetes Obes Metab. 2016 Dec;18(12):1176-1190.

2. Ambery PD, et al. Br J Clin Pharmacol. 2018 Oct;84(10):2325-2335.

3. Ambery P, et al. Lancet. 2018 Jun 30;391(10140):2607-2618.

4. Boland ML, et al. Nat Metab. 2020 May;2(5):413-431.

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