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Elagolix sodium

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Chemical Structure| 832720-36-2 同义名 : NBI-56418 sodium;Elagolix (sodium salt);ABT-620;NBI-56418
CAS号 : 832720-36-2
货号 : A136268
分子式 : C32H29F5N3NaO5
纯度 : 98%
分子量 : 653.572
MDL号 : MFCD12546649
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(76.5 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(76.5 mM)
动物实验配方：
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].
实验方案
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
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.