| Identification | Back Directory | [Name]
13-Oxa-2,4,10-triazapentadec-2-enoic acid, 15-[[(1R)-7-[(4'-carboxy-2-fluoro[1,1'-biphenyl]-4-yl)oxy]-1,2,3,4-tetrahydro-1-methyl-1-[2-oxo-2-(2-thiazolylamino)ethyl]-6-isoquinolinyl]oxy]-3,8-bis[[(1,1-dimethylethoxy)carbonyl]amino]-9-oxo-, 1-(1,1-dimethylethyl) ester, (2Z,8R)- | [CAS]
2216703-12-5 | [Synonyms]
13-Oxa-2,4,10-triazapentadec-2-enoic acid, 15-[[(1R)-7-[(4'-carboxy-2-fluoro[1,1'-biphenyl]-4-yl)oxy]-1,2,3,4-tetrahydro-1-methyl-1-[2-oxo-2-(2-thiazolylamino)ethyl]-6-isoquinolinyl]oxy]-3,8-bis[[(1,1-dimethylethoxy)carbonyl]amino]-9-oxo-, 1-(1,1-dimethylethyl) ester, (2Z,8R)- | [Molecular Formula]
C53H69FN8O13S | [MOL File]
2216703-12-5.mol | [Molecular Weight]
1077.22 |
| Hazard Information | Back Directory | [Uses]
(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor[1]. | [References]
[1] Petrilli WL, et al. From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9. Cell Chem Biol. 2019 Oct 22. pii: S2451-9456(19)30322-8. DOI:10.1016/j.chembiol.2019.10.002 |
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