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.
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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]. |
Dose | Monkey: 30 mg/kg[1] (p.o.) Beagle Dog: 10 mg/kg - 150 mg/kg[2] (p.o.) Rat: 300 mg/kg - 1200 mg/kg[2] (p.o.) |
Administration | p.o. |
Pharmacokinetics |
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 |
CAS号 | 832720-36-2 |
分子式 | C32H29F5N3NaO5 |
分子量 | 653.57 |
SMILES Code | O=C([O-])CCCN[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O.[Na+] |
MDL No. | MFCD12546649 |
别名 | NBI-56418 sodium; Elagolix (sodium salt); ABT-620; NBI-56418 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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