TAK-683 acetate |
| رقم الكتالوجGC62401 |
TAK-683 أسيتات هو ناهض كامل لمستقبل KISS1 (KISS1R) (IC50 = 170 pM) مع تحسين الاستقرار الأيضيTAK-683 أسيتات هو نظير ميتاستين غير ببتيد ، يعرض أنشطة ناهضة لـ KISS1R بقيم EC50 تبلغ 0.96 نانومتر و 1.6 نانومتر للإنسان والجرذان ، على التوالييستنفد خلات TAK-683 GnRH في منطقة ما تحت المهاد ويقلل من مستويات هرمون FSH و LH ومستويات هرمون التستوستيرون في الجسم الحي ، ولديه القدرة على دراسة سرطان البروستاتا المعتمد على الهرمونات
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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 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].
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].
[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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