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  2. GPCR/G Protein
  3. GnRH Receptor
  4. Relugolix

Relugolix  (Synonyms: 瑞盧戈利; TAK-385)

目錄號(hào): HY-16474 純度: 99.95%
COA 產(chǎn)品使用指南 技術(shù)支持

Relugolix (TAK-385) 是一種有效的，具有口服活性，非肽性促性腺激素釋放激素(GnRH) 的拮抗劑。與 TAK-013 (HY-100209 ) 相比，Relugolix 對(duì)人 (IC50=0.33 nM) 和猴子 (IC50=0.32 nM) 的受體具有高親和力和強(qiáng)拮抗活性。Relugolix 用于性激素依賴性疾病的研究，如子宮內(nèi)膜異位癥、子宮肌瘤、前列腺癌等。

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Relugolix Chemical Structure

Relugolix Chemical Structure

CAS No. : 737789-87-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥933
In-stock
5 mg ￥680
In-stock
10 mg ￥980
In-stock
25 mg ￥1750
In-stock
50 mg ￥2800
In-stock
100 mg ￥4200
In-stock
500 mg 現(xiàn)貨 詢價(jià)
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Relugolix:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].

IC50 & Target

IC50: 0.33 nM (human GnRH)
IC50: 0.32 nM (monkey GnRH)[2]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.08 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
[PMID: 21657270]
CHO IC50
0.32 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
[PMID: 21657270]
CHO IC50
0.32 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
[PMID: 21657270]
CHO IC50
0.33 nM
Compound: 16b, TAK-385
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
[PMID: 21657270]
CHO IC50
0.33 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
[PMID: 21657270]
CHO IC50
0.33 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
[PMID: 21657270]
CHO IC50
0.82 nM
Compound: 16b, TAK-385
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p
[PMID: 21657270]
CHO IC50
1700 nM
Compound: 16b, TAK-385
Antagonist activity at monkey GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in
Antagonist activity at monkey GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in
[PMID: 21657270]
CHO IC50
18 nM
Compound: 16b, TAK-385
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p
[PMID: 21657270]
CHO IC50
9800 nM
Compound: 16b, TAK-385
Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
[PMID: 21657270]
體外研究
(In Vitro)

Relμgolix 對(duì)猴子受體的結(jié)合親和力 (IC50=0.32 nM) 與對(duì)人受體的結(jié)合親和力 (IC50=0.33 nM) 相當(dāng)，同時(shí)顯示出 30000 倍降低大鼠受體 (IC50=9800 nM)。TAK-385 對(duì)人受體的體外拮抗活性 (IC90=18 nM) 超過猴受體 (IC90=1700 nM) 在 40% 血清存在時(shí)為 95 倍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Relμgolix (oral；1-3 mg/kg；single dose) 在 1 mg/kg 的劑量下表現(xiàn)出良好的藥代動(dòng)力學(xué)特征和明顯的循環(huán) LH 水平抑制作用。藥代動(dòng)力學(xué)特征顯示 Cmax、Tmax 和 AUCo 分別為 16.0 ng/mL、2.7 h 和 90.1 ng雄性食蟹猴[1]。
Relμgolix (oral；3、10或30 mg/kg；每日2次；4周) 顯著降低睪丸重量，并降低腹側(cè)前列腺重量在雄性 hGNRHR 敲入小鼠中，3 mg/kg 并在 10 mg/kg 時(shí)將其降低至去勢(shì)水平[2]。
Relμgolix (oral；30、100 或 200 mg /kg；每天兩次；4 周) 以 100 mg/kg 劑量在第一周內(nèi)在所有小鼠中誘導(dǎo)恒定的雌性間期，并在雌性 hGNRHR 敲入小鼠中在 4 周后以該劑量顯著降低卵巢和子宮的重量[2]。

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

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

Formula

C29H27F2N7O5S
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

瑞盧戈利
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (160.35 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.83 mg/mL (1.33 mM); 澄清溶液

    此方案可獲得 ≥ 0.83 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 8.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.83 mg/mL (1.33 mM); 澄清溶液

    此方案可獲得 ≥ 0.83 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 8.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.95%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6035 mL 8.0176 mL 16.0351 mL 40.0879 mL
5 mM 0.3207 mL 1.6035 mL 3.2070 mL 8.0176 mL
10 mM 0.1604 mL 0.8018 mL 1.6035 mL 4.0088 mL
15 mM 0.1069 mL 0.5345 mL 1.0690 mL 2.6725 mL
20 mM 0.0802 mL 0.4009 mL 0.8018 mL 2.0044 mL
25 mM 0.0641 mL 0.3207 mL 0.6414 mL 1.6035 mL
30 mM 0.0535 mL 0.2673 mL 0.5345 mL 1.3363 mL
40 mM 0.0401 mL 0.2004 mL 0.4009 mL 1.0022 mL
50 mM 0.0321 mL 0.1604 mL 0.3207 mL 0.8018 mL
60 mM 0.0267 mL 0.1336 mL 0.2673 mL 0.6681 mL
80 mM 0.0200 mL 0.1002 mL 0.2004 mL 0.5011 mL
100 mM 0.0160 mL 0.0802 mL 0.1604 mL 0.4009 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Relugolix
目錄號(hào)：
HY-16474
需求量：