Chemical Structure : 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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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.
分子量 | 616.02 | |
分子式 | C33H24ClF2N3O5 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Guangxin Dong, et al. J Med Chem. 2025 Apr 21. doi: 10.1021/acs.jmedchem.5c00242.
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