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Referencia número: HY-P2161

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TAK-683

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

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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No. CAS: 872719-49-8
Fòrmula: C₆₄H₈₃N₁₇O₁₃
Peso molecular:1298.45

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

TAK-683 Chemical Structure

No. CAS: 872719-49-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Pureza y Documentación
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Bioz

Actividad biológica

Descripciòn

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].

IC₅₀ & Target

IC50: 170 pM (metastin/GPR54)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.33 nM Compound: 22	Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay Agonist activity at human KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay	[PMID: 24918545]
CHO	EC₅₀	1.3 nM Compound: 22	Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay Agonist activity at rat KISS1R transfected in CHO cells assessed as intracellular calcium flux after 24 hrs by functional FLIPR assay	[PMID: 24918545]

In Vitro

TAK-683 exhibits an IC₅₀ value (95% CI) from receptor binding assays is 150-180 pM and EC₅₀ value (95% CI) from Ca⁺ mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TAK-683 (subcutaneous injection; 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^[3].
TAK-683 (subcutaneous injection; 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^[3].
TAK-683 (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male SD rat with prostate cancer model^[4]
Dosage:

2.1, 7, 14, 21 nmol/kg/day
Administration:

Subcutaneous injection
Result:

Exhibited a sustained testosterone suppression in rat.

Chemical Information

No. CAS 872719-49-8
Peso molecular 1298.45
Fòrmula C₆₄H₈₃N₁₇O₁₃
Sequence

N-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
Sequence Shortening

N-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW-NH2
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (4)

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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
Small Rumin Res

2024 Sep.

Pureza y Documentación

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Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (265 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

[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. [Content Brief]

[4]. Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions

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TAK-683

4 Cited Publications

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Pureza y Documentación
Referencias

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TAK-683

Publications Citing Use of MedChemExpress (MCE) TAK-683

Actividad biológica

Chemical Information

Publications (4)

Pureza y Documentación

Referencias

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TAK-683 Related Classifications

HY-P2161 Related Classifications