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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-DA-302168S
DA-302168S

Chemical Structure : DA-302168S

CAS No.: 2969158-02-7

DA-302168S

货号: PC-24419Not For Human Use, Lab Use Only.

DA-302168S is a potent, selective and orally bioavailable agonist of GLP-1R with EC50 of 1.32 nM in luciferase assay in HEK293 cells expressing hGLP-1R.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DA-302168S is a potent, selective and orally bioavailable agonist of GLP-1R with EC50 of 1.32 nM in luciferase assay in HEK293 cells expressing hGLP-1R.
DA-302168S does not activate GIPR, GLP-2R and GCGR at 10 uM.
DA-302168S activates GLP-1R of monkeys and humans, and exhibits little excitatory effect on GLP-1R of rats, mice, and dogs in a cAMP accumulation assay.
DA-302168S acts as a weak partial agonist in activating the β-arrestin pathway.
DA-302168S demonstrates superior in vitro and in vivo pharmacodynamics compared to Danuglipron and exhibits favorable pharmacokinetic (PK) properties and safety with an hERG IC50 value >30 μM.
DA-302168S is a promising therapeutic option for the management of T2D and obesity.

物理化学性质&存储条件

分子量 616.02
分子式 C33H24ClF2N3O5
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

(S)-2-(4-(6-((4-Chlorobenzofuran-7-yl)methoxy)-5-fluoropyridin-2-yl)-2-fluorobenzyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic Acid

参考文献

1. Guangxin Dong, et al. J Med Chem. 2025 Apr 21. doi: 10.1021/acs.jmedchem.5c00242.

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