恶拉戈利钠 /Elagolix sodium
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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 化学结构
Elagolix sodium 3D分子结构
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Elagolix sodium 质控信息
Elagolix sodium 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 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 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 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 技术信息
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