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TAK-683 TFA (872719-49-8 free base)

Catalog No. TP2156 CAS TP2156

Synonyms: TAK-683 TFA

TAK-683 TFA is a potent full agonist of the KISS1 receptor (KISS1R; IC50: 170 pM) with improved metabolic stability. It shows agonistic activities to KISS1R (EC50s: 0.96 nM and 1.6 nM for human and rat).

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TAK-683 TFA (872719-49-8 free base) Chemical Structure

TAK-683 TFA (872719-49-8 free base), CAS TP2156

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Description	TAK-683 TFA is a potent full agonist of the KISS1 receptor (KISS1R; IC50: 170 pM) with improved metabolic stability. It shows agonistic activities to KISS1R (EC50s: 0.96 nM and 1.6 nM for human and rat).
Targets&IC50	KISS1R:170 pM
In vivo	TAK-683 (s.c.; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer. TAK-683 (s.c.; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced. TAK-683 (s.c.; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA are reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14 [1].

Synonyms	TAK-683 TFA
Molecular Weight	1412.47
Formula	C66H84F3N17O15
CAS No.	TP2156

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Tanaka A, et al. Evaluation of pharmacokinetics/pharmacodynamics and efficacy of one-month depots of TAK-448 and TAK-683, investigational kisspeptin analogs, in male rats and an androgen-dependent prostate cancer model.Eur J Pharmacol. 2018 Mar 5;822:138-146. 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. 3. 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. 4. 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.

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Keywords

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