| Bioactivity | Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM. | ||||||
| Target | IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH) | ||||||
| Invitro | 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]. | ||||||
| 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[1]. | ||||||
| Name | Sufugolix | ||||||
| CAS | 308831-61-0 | ||||||
| Formula | C36H31F2N5O4S | ||||||
| Molar Mass | 667.72 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage |
*该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
||||||
| Reference | [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 |
Sufugolix
CAS: 308831-61-0 F: C36H31F2N5O4S W: 667.72
Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antago
Data collection：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.