kiss1r

TAK-448 acetate (MVT-602 acetate) 是一种小分子 KISS1R 激动剂，是一种和 kisspeptin 类似的合成肽。TAK-448 acetate 具有抗肿瘤活性，抑制 VCaP 细胞增殖，可用于研究前列腺癌。

TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).

TAK-683 TFA is a potent full agonist of the KISS1 receptor (KISS1R; IC50: 170 pM) with improved metabolic stability. It shows agonistic activities to KISS1R (EC50s: 0.96 nM and 1.6 nM for human and rat).

KISS1-305, the Metastin Kisspeptin analog, is a prototype peptide and chemical probe with suboptimal KISS1R agonistic activity and resistance to plasma protease degradation.

TAK-448 (MVT-602), a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM, has been studied in trials for the treatment of Prostate Cancer, Low Testosterone, Prostatic Neoplasms, and Hypogonadotropic Hypogonadism.

TAK-683 acetate是一种高效的KISS1R激动剂(IC50=170 pM)，改善了代谢稳定性。作为九肽metastin的类似物，对人和大鼠的EC50值分别为0.96 nM和1.6 nM。该化合物通过消耗下丘脑GnRH，能够降低血浆FSH、LH、睾酮水平，展示了对研究激素依赖性前列腺癌的潜力。