Elagolix sodium/恶拉戈利钠
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货号：A136268
同义名：
NBI-56418 sodium; Elagolix (sodium salt)
Elagolix sodium is an antagonist of human GnRH receptor (GnRHR) with IC50 and Ki of 0.25 nM and 3.7 nM, respectively.
Elagolix sodium/恶拉戈利钠 化学结构
Elagolix sodium/恶拉戈利钠 3D分子结构
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Elagolix sodium/恶拉戈利钠 纯度/质量文件 产品仅供科研
货号：A136268
标准纯度：
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Elagolix sodium/恶拉戈利钠 质控信息
Elagolix sodium/恶拉戈利钠 生物活性
描述
Elagolix Sodium is a sodium form of Elagolix. Elagolix is a potent nonpeptide GnRHR (gonadotropin-releasing hormone receptor) antagonist and may be potential to the treatment of endometriosis. It exhibited affinity to hGnRHR with Ki value of 0.9nM and inhibited GnRH (6 nM) stimulated inositol phosphate (IP) production with IC50 value of 1.5nM. Oral administration of Elagolix at 30mg/kg suppressed luteinizing hormone in castrated male cynomolgus macaques[3]
Elagolix sodium/恶拉戈利钠 动物研究
Dose
Monkey: 30 mg/kg[1] [2] [2]
Administration
p.o.
Pharmacokinetics
Animal
Rats[1]
Dogs[1]
Dose
10 mg/kg
50 mg/kg
Administration
i.v. or p.o.
p.o.
F
0.058
1
Vd
2.6 L/kg
0.92 L/kg
T1/2
0.9 h
2.8 h
Tmax
0.25 h
2 h
CLp
33.3 ml/min/kg
14.5 ml/min/kg
Cmax
338 ng/ml
13900 ng/ml
AUC0→∞
80700 ng/(ml·h)
AUC
290 ng/(ml·h)
Elagolix sodium/恶拉戈利钠 参考文献
[1] Chen C, Wu D, et al. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85.
[2] ELAGOLIX SODIUM
[3] Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454. PMID: 19006286.
Elagolix sodium/恶拉戈利钠 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.53mL
0.31mL
0.15mL
7.65mL
1.53mL
0.77mL
15.30mL
3.06mL
1.53mL
Elagolix sodium/恶拉戈利钠 技术信息
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