872719-49-8
Chemical Structure
TAK-683
- CAS No.: 872719-49-8
- Formula:C64H83N17O13
- Molecular Weight:1298.45
InChIKey: BDPDXFSIFWZPCE-PHOVXGMNSA-N
SMILES: O=C(N)[C@H](CC1=CNC2=C1C=CC=C2)NC([C@H](CCCNC(NC)=N)NC([C@H](CC(C)C)NC(NNC([C@H](CC3=CC=CC=C3)NC([C@H]([C@H](O)C)NC([C@H](CC(N)=O)NC([C@@H](CC4=CNC5=C4C=CC=C5)NC([C@@H](CC6=CC=C(O)C=C6)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][4].
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TAK-683 | TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer. | |||||||||||||||||||||
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References
- [1]. Nishizawa N, et al. Design 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. J Med Chem. 2016 Oct 13;59(19):8804-8811. Epub 2016 Sep 21. [Content Brief]
- [2]. Asami T, et al.Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.J Med Chem. 2013 Nov 14;56(21):8298-307. [Content Brief]
- [4]. Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions
