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 is a potent full KISS1 receptor (KISS1R) agonist (IC 50 =170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC 50 values of 0.96 nM and 1.6 nM for human and rat, respectively. 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.

Solid

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

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.
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.
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.
has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

N-Acetyl-YWNTF{aza}L{Met-R}W-NH2

[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.

In Vitro: H₂O : 5 mg/mL (3.68 mM; Need ultrasonic)配制储备液