Elagolix Sodium

目录号:S4896 别名: NBI-56418, ABT-620

Elagolix Sodium Chemical Structure

Molecular Weight(MW): 653.57

Elagolix Soidum是一种有效的、选择性的、具有口服活性的促性腺激素释放激素受体GnRHR非肽段拮抗剂,Kd值为54 pM。浓度为10 μM时,对离子通道、酶和转运体没有显著的活性作用(inhibition <50%)。

规格 价格 库存 购买数量  
RMB 876.81 现货
RMB 2211.31 现货
RMB 5217.99 现货
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Estrogen/progestogen Receptor抑制剂选择性比较

生物活性

产品描述 Elagolix Soidum是一种有效的、选择性的、具有口服活性的促性腺激素释放激素受体GnRHR非肽段拮抗剂,Kd值为54 pM。浓度为10 μM时,对离子通道、酶和转运体没有显著的活性作用(inhibition <50%)。
靶点
GnRHR [1]
(Cell-free assay)
54 pM(Kd)
体外研究

Elagolix displays high affinity in a competition binding assay for hGnRH-R (Ki = 0.90 nM) and low CYP3A4 inhibition (IC50 = 56 μM). It is a slowly disassociating antagonist exhibiting very high affinity (KD = 54 pM) and insurmountable antagonism. Elagolix is highly selective at hGnRH-R, its wider receptor selectivity is tested at a concentration of 10 μM in a panel of radioligand binding assays for 100 off-target receptors, ion channels, enzymes, and transporters, and significant activity is not observed (inhibition <50%). It does not stimulate histamine release from cultured rat peritoneal mast cells. Elagolix lacks the necessary high binding affinity to the rat GnRH receptor (Ki = 4400 nM) and it possesses high affinity at the monkey GnRH receptor (Ki = 3.3 nM)[1].

体内研究 Oral administration of Elagolix suppresses luteinizing hormone in castrated macaques. Elagolix shows good efficacy in suppressing luteinizing hormone in monkeys and exhibits high oral bioavailability in dogs (~100% when dosed via oral gavage at 50 mg/kg)[1].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: RBL-1 cells stably expressing the human cloned GnRH receptor
  • Concentrations: --
  • Incubation Time: 1 h
  • Method:

    RBL-1 cells stably expressing the human cloned GnRH receptor are seeded into 96 well plates at a density of 15 000 cells per well in inositol-free DMEM containing 10% dialyzed FBS, 10 mM HEPES, 2 mM L-glutamine, 1 mM sodium pyruvate, 0.1 mM nonessential amino acids, and 50 μg/mL penicillin/streptomycin and are labeled for 48 h with 0.2 μCi myo-2-[3H]inositol. The cells are washed once in PBS and pretreated with assay buffer (140 mM NaCl, 4 mM KCl, 20 mM HEPES, 8.3 mM glucose, 1 mM MgCl2, 1 mM CaCl2, 10 mM LiCl, and 0.1% BSA) for 15-60 min at 37 °C. The cells are then stimulated with GnRH (6 nM) in the presence or absence of antagonist and incubated for 60 min at 37℃. Cells are extracted with 10 mM formic acid at 4℃ for 30 min, and the lysate is loaded onto Millipore plates containing 20 μg of Dowex AG1-X8 resin. The plate is washed once in H2O and once in 60 mM ammonium formate/5 mM sodium tetraborate, and inositol phosphates are eluted with 1 M ammonium formate/0.1 M formic acid. The eluate is transferred to a Lumaplate and counted in a TopCount NXT.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: Rhesus Monkey
  • Formulation: water or 5% cromophore (For i.v. formulation); a sterile water solution (For oral formulation)
  • Dosages: 10 and 50 mg/kg (oral); 3 and 10 mg/kg (i.v.)
  • Administration: p.o. or i.v.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (153.0 mM)
Water 100 mg/mL (153.0 mM)
Ethanol 100 mg/mL (153.0 mM)

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 653.57
化学式

C32H29F5N3O5.Na

CAS号 832720-36-2
储存条件 粉状
溶于溶剂
别名 NBI-56418, ABT-620

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID