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TAK-683

CAT: 0804-HY-P2161Size: 1 EachDry Ice: NoHazardous: No
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Description
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].
CAS Number
872719-49-8
UNSPSC
12352209
Target
Kisspeptin Receptor
Type
Peptides
Related Pathways
GPCR/G Protein
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/tak-683.html
Solubility
10 mM in DMSO
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
Molecular Formula
C64H83N17O13
Molecular Weight
1298.45
References & Citations
[1]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.|[2]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.|[3]Matsui H, et al. Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.Eur J Pharmacol. 2014 Jul 15;735:77-85.|[4]Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions
Shipping Conditions
Room temperature
Scientific Category
Peptides
Clinical Information
Phase 1

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