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Relugolix
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。
Relugolix图片
CAS NO:737789-87-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
瑞卢戈利
TAK-385
产品介绍
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 (HY-100209 ) 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。
生物活性

Relugolix (TAK-385) is a potent, orally active, nonpeptidicgonadotropin-releasing hormone (GnRH)antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (bindingIC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostatecanceret al[2].

IC50& Target

IC50: 0.33 nM (human GnRH)
IC50: 0.32 nM (monkey GnRH)[2]

体外研究
(In Vitro)

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[1].

体内研究
(In Vivo)

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 Cmax, Tmax, and AUCo, respectively in male cynomolgus monkeys[1].
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[2].
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[2].

Animal Model:Male hGNRHR-knock-in mice[2]
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[2]
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.
Clinical Trial
分子量

623.63

性状

Solid

Formula

C29H27F2N7O5S

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.6035 mL8.0176 mL16.0351 mL
5 mM0.3207 mL1.6035 mL3.2070 mL
10 mM0.1604 mL0.8018 mL1.6035 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。

*以上所有助溶剂都可在本网站选购。