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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
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | castrated male cynomolgus monkeys |
| Formulation | -- |
| Dosages | 30 mg / kg |
| Administration | p.o. |
| Molecular Weight | 667.72 |
| Formula | C36H31F2N5O4S |
| CAS Number | 308831-61-0 |
| Solubility (25°C) | 10mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Szkudlinski MW Mol Pharmacol. Challenges and opportunities of trapping ligands.
| Related LHRH/GnRH Products |
|---|
| Goserelin acetate
Goserelin acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist), also known as a luteinizing hormone releasing hormone (LHRH) agonist. |
| Deslorelin Acetate
Deslorelin is an injectable gonadotropin releasing hormone super-agonist (GnRH agonist) also known as an LHRH agonist. |
| Alarelin Acetate
Alarelin acetate is a synthetic GnRH agonist. Alarelin is found in higher amounts than that of LH-RH in rat hypophyseal stimulation of gonadotropin secretion in vivo and in vitro and in ovulation inductions. |
| Leuprolide Acetate
Leuprolide acetate is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors. |
| Relugolix
Relugolix, also known as TAK-385, is an orally active gonadotropin-releasing hormone (GnRH) antagonist with an IC50 of 0.12 nM. |
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