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恶拉戈利钠 /Elagolix sodium {[allProObj[0].p_purity_real_show]}

货号:A136268 同义名: NBI-56418 sodium;Elagolix (sodium salt) Ambeed 开学季,买赠积分,赢豪礼

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 CAS号:832720-36-2
Elagolix sodium 化学结构
CAS号:832720-36-2
Elagolix sodium 3D分子结构
CAS号:832720-36-2
Elagolix sodium 化学结构 CAS号:832720-36-2
Elagolix sodium 3D分子结构 CAS号:832720-36-2
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Elagolix sodium 纯度/质量文件 产品仅供科研

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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] (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
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
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

CAS号832720-36-2
分子式C32H29F5N3NaO5
分子量 653.572
别名 NBI-56418 sodium;Elagolix (sodium salt);ABT-620;NBI-56418
运输蓝冰
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
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