TAK-683 acetate|西域试剂

TAK-683 acetate,98.97%

产品编号：Bellancom-P2161B| 分子式：C₆₆H₈₇N₁₇O₁₅| 分子量：1358.50

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货号	价格	库存与货期
Bellancom-P2161B	￥3500.00	杭州北京（现货）
Bellancom-P2161B	￥8500.00	杭州北京（现货）
Bellancom-P2161B	￥14500.00	杭州北京（现货）

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TAK-683 acetate

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 full KISS1 receptor (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀ values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer^[4].

体外研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	0.7361 mL	3.6805 mL	7.3611 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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