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TAK-683 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TAK-683 TFA图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TAK-683 TFA 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 TFA 是一个九肽 metastin 的类似物,对 KISS1R 具有激动作用,针对人与大鼠EC50值分别为 0.96 nM 和 1.6 nM。 TAK-683 TFA 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。
生物活性

TAK-683 TFA is a potent fullKISS1 receptor (KISS1R)agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R withEC50values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasmaFSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostatecancer[1][2][3].

IC50& Target

IC50: 170 pM (metastin/GPR54)[1]

体内研究
(In Vivo)

TAK-683 (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[1].
TAK-683 (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[1].
TAK-683 (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[1].

Animal Model:Male SD rat with prostate cancer model[1]
Dosage:2.1, 7, 14, 21 nmol/kg/day
Administration:Subcutaneous injection
Result:Exhibited a sustained testosterone suppression in rat.
分子量

1412.47

Formula

C66H84F3N17O15

Sequence Shortening

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.