Powder: -20°C for 3 years
In solvent: -80°C for 2 years
TAK-013 is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor.
Description | TAK-013 is a potent and orally available luteinizing hormone-releasing hormone LHRH receptor. |
Targets&IC50 | LHRH:0.1 nM. |
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. It is observed that the cis conformer of the methoxyurea is more populated than the trans conformer by high-temperature molecular dynamics calculation during the conformational analysis of sufugolix[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). Sufugolix has the apparent lipophilicity to allow increased membrane permeability and consequently improve its oral absorption in monkeys. 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]. |
Kinase Assay | The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1]. |
Synonyms | TAK-013 |
Molecular Weight | 667.73 |
Formula | C36H31F2N5O4S |
CAS No. | 308831-61-0 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 10mM
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Sufugolix 308831-61-0 内分泌与激素 LHRH TAK 013 TAK-013 Inhibitor inhibit TAK013 inhibitor