67482-10-4

Basic information

• Product Name: 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzoicacid
• Synonyms: 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzoicacid;EOS-60449
• CAS NO: 67482-10-4
• Molecular Formula: C₁₂H₈N₄O₂
• Molecular Weight: 240.22
• Mol File: 67482-10-4.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzoicacid(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzoicacid(67482-10-4)
• EPA Substance Registry System: 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzoicacid(67482-10-4)

Safety Data

• Hazardous Substances Data: 67482-10-4(Hazardous Substances Data)

Upstream product

• 78750-69-3 ethyl 4-((3-aminopyridin-2-yl)amino)benzoate 
• 78750-62-6 ethyl 4-((3-nitropyridin-2-yl)amino)benzoate 
• 94-09-7 p-aminoethylbenzoate 
• 5470-18-8 2-Chloro-3-nitropyridine 

Relevant articles and documents

Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain

Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the compound PF-06446846 inhibits translation of PCSK9 by inducing the ribosom

Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents

The optimization of a new class of small molecule PCSK9 mRNA translation inhibitors is described. The potency, physicochemical properties, and off-target pharmacology associated with the hit compound (1) were improved by changes to two regions of the molecule. The last step in the synthesis of the congested amide center was enabled by three different routes. Subtle structural changes yielded significant changes in pharmacology and off-target margins. These efforts led to the identification of 7l and 7n with overall profiles suitable for in vivo evaluation. In a 14-day toxicology study, 7l demonstrated an improved safety profile vs lead 7f. We hypothesize that the improved safety profile is related to diminished binding of 7l to nontranslating ribosomes and an apparent improvement in transcript selectivity due to the lower strength of 7l stalling of off-target proteins.

SUBSTITUTED AMIDE COMPOUNDS

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