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TAK-683 acetate
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 acetate图片
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

TAK-683 acetate is a potent fullKISS1 receptor (KISS1R)agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate 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 acetate 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][4].

体外研究
(In Vitro)

TAK-683 acetate exhibits an IC50value (95% CI) from receptor binding assays is 150-180 pM and EC50value (95% CI) from Ca+mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells[4].

体内研究
(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[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].

Animal Model:Male SD rat with prostate cancer model[4]
Dosage:2.1, 7, 14, 21 nmol/kg/day
Administration:Subcutaneous injection
Result:Exhibited a sustained testosterone suppression in rat.
分子量

1358.50

性状

Solid

Formula

C66H87N17O15

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

Sealed storage, away from moisture and light, under nitrogen

Powder-80°C2 years
-20°C1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据
In Vitro: 

H2O : 5 mg/mL(3.68 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.7361 mL3.6805 mL7.3611 mL
5 mM---------
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。