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

Sufugolix (TAK-013)高效有口服活性的黃體激素釋放激素 (LHRH) 受體拮抗劑，IC50值為0.1 nM。

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Sufugolix Chemical Structure

Sufugolix Chemical Structure

CAS No. : 308831-61-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥396
In-stock
5 mg ￥990
In-stock
10 mg ￥1650
In-stock
25 mg ￥3650
In-stock
50 mg 現(xiàn)貨 詢價(jià)
100 mg   詢價(jià)  
200 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.

IC50 & Target

IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.06 nM
Compound: 1
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
0.1 nM
Compound: 1
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
1.3 nM
Compound: 1
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
1.6 nM
Compound: 1
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
1.6 nM
Compound: 1
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
1.9 nM
Compound: 1
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
13694 nM
Compound: 1
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
270 nM
Compound: 1
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]
體外研究
(In Vitro)

Sufμgolix 對(duì)人類受體的選擇性分別超過猴子和大鼠受體的 3 倍和 2000 倍。Sufμgolix 有效拮抗表達(dá)人 (IC50=0.1 nM) 和猴 (IC50=0.6 nM) 受體的 CHO 細(xì)胞上的 LHRH 功能[1]。

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

在 30 mg/kg 的劑量下，Sufμgolix 的口服給藥幾乎完全抑制了閹割的雄性食蟹猴的血漿 LH 水平，并具有足夠的作用持續(xù)時(shí)間 (超過 24 小時(shí))。在 30 和 10 mg/kg 劑量下，Sufμgolix 的最大血漿濃度分別為 0.34 μM (給藥后 6 小時(shí)達(dá)到) 和 0.18 μM (給藥后 4 小時(shí)達(dá)到)[1]。

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

667.72

Formula

C36H31F2N5O4S
CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

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

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 20 mg/mL (29.95 mM; 超聲助溶 (<60°C); 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)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.4976 mL 7.4882 mL 14.9763 mL
5 mM 0.2995 mL 1.4976 mL 2.9953 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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

  • 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
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Kinase Assay
[1]

The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Monkeys: Sufugolix (10 or 30 mg/kg, 3 mL/kg, n=3 for each group) is suspended in 0.5% methylcellulose containing 1.2% citric acid, or 0.5% methylcellulose containing 1.2% citric acid alone (3 mL/kg, n=3), are administered orally. Blood samples (heparin-plasma) are collected from a femoral vein 24 h before administration and 0, 2, 4, 8, 24, and 48 h after administration. LH concentrations in the plasma are measured by bioassays using mouse testicular cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

Sufugolix 相關(guān)分類

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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4976 mL 7.4882 mL 14.9763 mL 37.4408 mL
5 mM 0.2995 mL 1.4976 mL 2.9953 mL 7.4882 mL
10 mM 0.1498 mL 0.7488 mL 1.4976 mL 3.7441 mL
15 mM 0.0998 mL 0.4992 mL 0.9984 mL 2.4961 mL
20 mM 0.0749 mL 0.3744 mL 0.7488 mL 1.8720 mL
25 mM 0.0599 mL 0.2995 mL 0.5991 mL 1.4976 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：
Sufugolix
目錄號(hào)：
HY-100209
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