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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-LSN3318839
LSN3318839

Chemical Structure : LSN3318839

CAS No.: 2764704-18-7

LSN3318839 (LSN 3318839)

货号: PC-20512Not For Human Use, Lab Use Only.

LSN3318839 is a potent, positive allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 14 nM, Emax of 104%.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LSN3318839 is a potent, positive allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R) with EC50 of 14 nM, Emax of 104%.
LSN3318839 increases the potency and efficacy of the weak metabolite GLP-1(9-36)NH2 to become a full agonist at the GLP-1R and modestly potentiates the activity of the highly potent full-length ligand, GLP-1(7-36)NH2.
LSN3318839 preferentially enhances G protein-coupled signaling by the GLP-1R over β-arrestin recruitment.
LSN3318839 demonstrates robust glucose lowering in animal models alone or in treatment combination with sitagliptin.

物理化学性质&存储条件

分子量 480.39
分子式 C26H23Cl2N3O2
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

O=C(O)[C@H](C)C1=CC=CC=C1C2=CC3=C(N=CN3[C@@H](C4=C(Cl)C=CC(C5CC5)=C4Cl)C)C=N2

参考文献

1. Francis S Willard, et al. J Med Chem. 2021 Mar 25;64(6):3439-3448.

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