TAK-683 acetate 

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].

TAK-683 acetate 在表达大鼠 kiss1r 的中国仓鼠卵巢（CHO）细胞中显示 IC₅₀ 值 为 150-180 pM 和 EC₅₀ 值 为 180 pM。

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

TAK-683 acetate (皮下注射；0.008、0.08、0.8 或 8 μMol/mL/kg；每天一次；7 天) 诱导血浆促黄体激素和睾酮水平升高；然而，在第 7 天后，血浆激素水平和生殖器官重量降低^[3]。
TAK-683 acetate (皮下注射；10、30 或 100 pmol/h；每天一次；4 周) 为抑制生殖功能和激素相关疾病如前列腺癌提供了前景^[3]。
TAK-683 acetate (皮下注射；2.1-21 nmol/kg/天；每天一次；12 周) 在前列腺癌模型中进行了长期评估，大鼠的血清 PSA 浓度降低，所有大鼠的 PSA 浓度均降低至检测限以下 (0.5 ng/mL)) 14^[4]。

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

1358.50

C₆₆H₈₇N₁₇O₁₅

固体

White to off-white

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

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

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

* 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 (sealed storage, away from moisture and light, 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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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