货号	规格	价格	上海	北京	珠海	重庆	武汉
S84864-1mg促销	≥98%	￥326.00 ￥294.00 S84864-1mg ￥294.00 现货	10 10	-	-	-	-
S84864-5mg促销	≥98%	￥822.00 ￥739.00 S84864-5mg ￥739.00 现货	9 9	-	-	-	-
S84864-10mg促销	≥98%	￥1370.00 ￥1230.00 S84864-10mg ￥1230.00 现货	5 5	-	-	-	-
S84864-25mg促销	≥98%	￥2970.00 ￥2670.00 S84864-25mg ￥2670.00 现货	2 2	-	-	-	-

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产品描述：

Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.

靶点：

IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH);LHRH

体外研究：

Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. During the conformational analysis of sufugolix, using high-temperature molecular dynamics calculation, it is observed that the cis conformer of the methoxyurea is more populated than the trans conformer。

体内研究：

Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively。

参考文献：

1. Sasaki S, et al. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J Med Chem. 2003 Jan 2;46(1):113-24.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.498 ml	7.488 ml	14.976 ml
5 mM	0.3 ml	1.498 ml	2.995 ml
10 mM	0.15 ml	0.749 ml	1.498 ml
50 mM	0.03 ml	0.15 ml	0.3 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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SUFUGOLIX