TAK-683 TFA
Based on 4 publication(s) in Google Scholar
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA 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 TFA 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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- Formule: C66H84F3N17O15
- Masse moléculaire:1412.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TAK-683 TFA
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Activité biologique
IC50: 170 pM (metastin/GPR54)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rat with prostate cancer model[1]
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Dosage:2.1, 7, 14, 21 nmol/kg/day
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Administration:Subcutaneous injection
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Result:Exhibited a sustained testosterone suppression in rat.
Chemical Information
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Masse moléculaire 1412.47
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Formule C66H84F3N17O15
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Sequence
N-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
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Sequence Shortening
N-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Anal Chem
A Computational Integration Strategy Driven by Chemical Similarity Uncovers Comprehensive Metabolic Profiles of Small Bioactive Peptides via UHPLC-HRMS for Doping Control. [Abstract]2025 Nov 18;97(45):25158-25167. PMID: 41202118 -
Anim Reprod Sci
Effect of post-mating TAK-683 (Kisspeptin analog) treatment on luteal morphology and function in suckling goats with lactational anestrus. [Abstract]2026 Jan:284:108052. PMID: 41343946 -
Vet Res Commun
First clinical use of the kisspeptin analog TAK-683 in the treatment of a follicular cyst in a goat: case report. [Abstract]2026 Mar 12;50(3):194. PMID: 41817855 -
Pureté et documentation
Références
[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. [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]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TAK-683 TFA Related Classifications
HY-P2161A Related Classifications
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