Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with anIC₅₀of 0.1 nM.

IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH)^[1]

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^[1].

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^[1].

667.72

Solid

C₃₆H₃₁F₂N₅O₄S

308831-61-0

Room temperature in continental US; may vary elsewhere.

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

DMSO : 1.25 mg/mL(1.87 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

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