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TAK-683 acetate

CAS No. :

MCE 站：TAK-683 acetate

产品活性：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。

研究领域：Others

作用靶点：Others

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.

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.
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.

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