包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
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].
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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
*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
* 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。 |