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Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM).
Relugolix (TAK-385) acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis.
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Animal models | Six-week-old male hGNRHR-knock-in mice |
Formulation | 0.5% methylcellulose solution containing 6 mg/mL citric acid monohydrate |
Dosages | 3, 10 or 30 mg/kg |
Administration | oral |
Molecular Weight | 623.63 |
Formula | C29H27F2N7O5S |
CAS Number | 737789-87-6 |
Solubility (25°C) | DMSO: ≥ 48 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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