Sufugolix

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sufugolix (TAK-013) 是一种高效、口服生物可利用的黄体生成素释放激素 (LHRH) 受体非肽拮抗剂，对人 LHRH 的结合和功能 IC50 分别为 0.1 和 0.06 nM。

Sufugolix (TAK-013) is a highly potent and orally bioavailable non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor with binding and functional IC50 of 0.1 and 0.06 nM for human LHRH, respectively; completely suppresses plasma LH levels in castrated male cynomolgus monkeys at 30 mg/kg dose with sufficient duration of action (>24 h)(In Vitro):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 .(In Vivo):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.

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 .

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.

TAK013 | TAK-013 | TAK 013

GPCR/G Protein

LHR

humanLHRH|monkeyLHRH

Other Indications

Other Disease

308831-61-0

667.7242

C36H31F2N5O4S

>98% (HPLC)

10 mM in DMSO

O=C(NOC)NC1=CC=C(C(S2)=C(CN(C)CC3=CC=CC=C3)C(C(N4C5=CC=CC=C5)=O)=C2N(CC6=C(F)C=CC=C6F)C4=O)C=C1

Urea, N-[4-[1-[(2,6-difluorophenyl)methyl]-1,2,3,4-tetrahydro-5-[[methyl(phenylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy-

(-20℃)

With Ice Pack

≥ 2 years