《Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Richard-Bildstein, Sylvia; Aissaoui, Hamed; Pothier, Julien; Schafer, Gabriel; Gnerre, Carmela; Lindenberg, Eleanor; Lehembre, Francois; Pouzol, Laetitia; Guerry, Philippe. COA of Formula: C10H20N2O2 The article mentions the following:
The chemokine receptor CXCR7, also known as ACKR3, is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies such as neurol. diseases, autoimmune diseases, and cancers. By binding and scavenging the chemokines CXCL11 and CXCL12, CXCR7 regulates their extracellular levels. From an original high-throughput screening campaign emerged an arylketoamide hit among others. The hit-to-lead optimization led to the discovery of a novel chemotype series of acylaminopiperidinecarboxamides. This series provided CXCR7 antagonists that block CXCL11- and CXCL12-induced ss-arrestin recruitment. Further structural modifications on the acylaminopiperidinecarboxamide framework yielded compounds with high CXCR7 antagonistic activities and balanced ADMET properties. The effort described herein culminated in the discovery of ACT-1004-1239 I. Biol. characterization of I demonstrated that it is a potent, insurmountable antagonist. Oral administration of I in mice up to 100 mg/kg led to a dose-dependent increase of plasma CXCL12 concentration In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7COA of Formula: C10H20N2O2)
tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.COA of Formula: C10H20N2O2
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem