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

Sufugolix  (Synonyms: TAK-013)

目录号: HY-100209 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

Sufugolix (TAK-013)高效有口服活性的黄体激素释放激素 (LHRH) 受体拮抗剂，IC50值为0.1 nM。

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Sufugolix Chemical Structure

Sufugolix Chemical Structure

CAS No. : 308831-61-0

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥396
In-stock
5 mg ￥990
In-stock
10 mg ￥1650
In-stock
25 mg ￥3650
In-stock
50 mg ￥6550
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Sufugolix 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

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]
体外研究
(In Vitro)

Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. During the conformational analysis of sufugolix, using high-temperature molecular dynamics calculation, it is observed that the cis conformer of the methoxyurea is more populated than the trans conformer [1].

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

Sufugolix 相关抗体:
体内研究
(In Vivo)

Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively[1].

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

667.72

Formula

C36H31F2N5O4S
CAS 号
性状

固体

颜色

Light yellow to yellow

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

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 20 mg/mL (29.95 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
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.
参考文献

Sufugolix 相关分类

完整储备液配制表

* 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

可选溶剂 浓度 溶剂体积 质量 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.

Keywords:

Sufugolix308831-61-0TAK-013TAK013TAK 013GnRH ReceptorGonadotropin releasing hormone receptorGNRHRInhibitorinhibitorinhibit

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目录号：
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