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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-YN1548
YN1548

Chemical Structure : YN1548

CAS No.: 2643967-34-2

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YN1548 (YN-1548)

货号: PC-25559Not For Human Use, Lab Use Only.

YN1548 is a potent, highly selective agonist of human glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 4.59, 24.28, and 2.20 nM in CHO cells expressing low, mid, and high human GLP-1 receptor levels in a dose-dependent manner, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

YN1548 is a potent, highly selective agonist of human glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 4.59, 24.28, and 2.20 nM in CHO cells expressing low, mid, and high human GLP-1 receptor levels in a dose-dependent manner, respectively.
YN1548 induces β-arrestin 2 translocation with an Emax of 40.0 %, demonstrates Emax comparable to GLP-1 (7–36) amide.
YN1548 is highly selective for GLP-1 receptor among the glucagon receptor family, does not activate cAMP response in CHO cells expressing GLP-2 receptor, GIP receptor, or glucagon receptor
YN1548 binding to cynomolgus monkey GLP-1 receptor expressed in CHO cells enhanced the intracellular cAMP concentration at an EC50 of 59.91 nM and an Emax of 101.5 %.
Oral administration of YN1548 reduced blood glucose levels and enhanced insulin secretion in a concentration-dependent manner in diabetic monkeys.

物理化学性质&存储条件

分子量 571.61
分子式 C30H30FN7O4
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
Chemical Name/SMILES

2-(((S)-4-(6-((4-cyano-2-fluorobenzyl)oxy)pyrazin-2-yl)-2-methylpiperazin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid

参考文献

1. Je IG, et al. YN1548: A novel small-molecule agonist of human glucagon-like peptide-1 receptor for the treatment of type 2 diabetes mellitus and obesity. Eur J Pharmacol. 2025 Sep 11;1006:178143.

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