TAK-683

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TAK-683 

TAK-683 是一种有效的完全 KISS1R 激动剂 (IC50=170 pM)，具有改善的代谢稳定性。TAK-683 是一个九肽 metastin 的类似物，针对人与大鼠 EC50 值分别为 0.96 nM 和 1.6 nM。TAK-683 消耗下丘脑 GnRH，降低血浆FSH、LH、睾酮水平，具有研究激素依赖性前列腺癌的潜力。

TAK-683

TAK-683 Chemical Structure

CAS No. : 872719-49-8

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TAK-683 的其他形式现货产品:

TAK-683 acetate

生物活性

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]
体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

1298.45

Formula

C64H83N17O13
CAS 号

872719-49-8
Sequence

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

N-Acetyl-YWNTF{aza}L{Met-R}W-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

    [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]. 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

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