TAK-683 acetate

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TAK-683 acetate 

TAK-683 acetate 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 acetate 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 acetate 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 acetate

TAK-683 acetate Chemical Structure

规格 价格 是否有货 数量
1 mg ￥3500 In-stock
5 mg ￥8500 In-stock
10 mg ￥14500 In-stock
50 mg   询价  
100 mg   询价  

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TAK-683 acetate 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate 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 acetate 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].

体外研究
(In Vitro)

TAK-683 acetate 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 acetate (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 acetate (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 acetate (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

1358.50

Formula

C66H87N17O15
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

Protect from light, stored under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro: 

H2O : 5 mg/mL (3.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7361 mL 3.6805 mL 7.3611 mL
5 mM — — —
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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]. Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions

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