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製品番号: HY-P2161

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TAK-683

4 Cited Publications

カスタマーレビュー

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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CAS 番号: 872719-49-8
分子式: C₆₄H₈₃N₁₇O₁₃
分子量:1298.45

保管条件:

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

TAK-683 構造式

CAS 番号: 872719-49-8

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Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (4)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 872719-49-8
分子量 1298.45
分子式 C₆₄H₈₃N₁₇O₁₃
配列

N-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
シーケンスの短縮

N-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW-NH2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (265 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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TAK-683

4 Cited Publications

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
Publications (4)
純度とドキュメンテーション
参考文献

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TAK-683

MedChemExpress（MCE）の使用を引用している文献 TAK-683

生物活性

化学情報

Publications (4)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

TAK-683 関連分類

HY-P2161 関連分類