Relugolix - CAS:737789-87-6

您当前的位置：

Relugolix (Synonyms:瑞卢戈利; TAK-385)

目录号 : KM9953 CAS No. : 737789-87-6 纯度 : 98%

Data Sheet 产品使用指南

Relugolix (TAK-385) 是一种有效的，具有口服活性，非肽性促性腺激素释放激素(GnRH) 的拮抗剂。与 TAK-013相比，Relugolix 对人 (IC50=0.33 nM) 和猴子 (IC50=0.32 nM) 的受体具有高亲和力和强拮抗活性。Relugolix 用于性激素依赖性疾病的研究，如子宫内膜异位症、子宫肌瘤、前列腺癌等。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

查看所有商品（2）

加入购物车大包装询价

Other Forms of Rapamycin:

Ganirelix Acetate In-stock
Buserelin Acetate In-stock
Triptorelin acetate In-stock
Alarelin Acetate In-stock
Cetrorelix Acetate In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC₅₀=0.33 nM) and monkey receptor (IC₅₀=0.32 nM) compared with TAK-013 . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.

体外研究

Relugolix exhibits strong binding affinity (IC₅₀=0.32 nM) for the monkey receptor comparable to that for the human receptor (IC₅₀=0.33 nM) while displaying a 30000-fold decrease for the rat receptor (IC₅₀=9800 nM). The antagonistic in vitro activity of TAK-385 with respect to the human receptor (IC₉₀=18 nM) exceeded that for the monkey receptor (IC₉₀=1700 nM) by 95-fold in the presence of 40% serum.

体内研究

Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) exhibits a good pharmacokinetic profile and obvious suppressive effects of circulating LH levels in monkeys at a dose of 1 mg/kg. The pharmacokinetic profile exhibits with 16.0 ng/mL, 2.7 h, and 90.1 ng for C_max, T_max, and AUC_o, respectively in male cynomolgus monkeys.
Relugolix (oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks) significantly decreases the testis weight, and reduces the ventral prostate weight at 3 mg/kg and decreases it to castrate levels at 10 mg/kg in male hGNRHR-knock-in mice.
Relugolix (oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks) induces constant diestrous phases in all mice within the first week at 100 mg/kg, and significantly decreases the weights of ovaries and uteri at this dose after 4 weeks in female hGNRHR-knock-in mice.

Animal Model:	Male hGNRHR-knock-in mice
Dosage:	3, 10 or 30 mg/kg
Administration:	Oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks
Result:	Decreased testicular function.

Animal Model:	Female hGNRHR-knock-in mice
Dosage:	30, 100 or 200 mg/kg
Administration:	Oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks
Result:	Suppressed the hypothalamic–pituitary–gonadal axis to gonadectomized levels. Downregulated GnRH receptor mRNA levels in the pituitary.

分子式

C₂₉H₂₇F₂N₇O₅S

分子量

623.63

CAS号

737789-87-6

中文名称

瑞卢戈利

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (160.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6035 mL	8.0176 mL	16.0351 mL
5 mM	0.3207 mL	1.6035 mL	3.2070 mL
10 mM	0.1604 mL	0.8018 mL	1.6035 mL

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.33 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

临床试验

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation