Nishizawa, Naoki published the artcileDesign and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-D-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility, SDS of cas: 158922-07-7, the main research area is nonapeptide KISS1 receptor agonist testosterone.
Metastin/kisspeptin is an endogenous ligand of KISS1R. Metastin and KISS1R are suggested to play crucial roles in regulating the secretion of GnRH and continuous administration of metastin derivatives attenuated the plasma testosterone levels in male rats. The optimization studies of metastin derivatives led to the discovery of Ac-D-Tyr-D-Trp-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2, TAK-683, (I), which suppressed plasma testosterone in rats at lower doses than those of leuprolide. Although I possessed an extremely potent pharmacol. activity, 20-mg/mL aqueous solution of I has a gel formation property. In order to improve this physicochem. property, the authors substituted D-Trp at position 47 with a variety of amino acids; the authors identified that substitution with cyclic amino acids, which could change peptide conformation, retained its potency. Especially, Hyp47 analog TAK-448 (II) showed not only superior pharmacol. activity to I, but also excellent water solubility Furthermore, 20-mg/mL aqueous solution of 24 did not show a gel formation up to five days.
Journal of Medicinal Chemistry published new progress about Homo sapiens. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, SDS of cas: 158922-07-7.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem