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Cat. No. M9197
Relugolix Structure

Orgovyx; TAK-385; RVT-601

Size Price Availability Quantity
5mg USD 133  USD133 In stock
10mg USD 209  USD209 In stock
50mg USD 733  USD733 In stock
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Quality Control
Biological Activity

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.

Cell Experiment
Cell lines
Preparation method
Incubation time
Animal Experiment
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 623.63
Formula C29H27F2N7O5S
CAS Number 737789-87-6
Purity >98.5%
Solubility DMSO: ≥ 48 mg/mL
Storage at -20°C

[1] MacLean DB, et al. J Clin Endocrinol Metab. Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males.

[2] Nakata D, et al. Eur J Pharmacol. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice.

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Keywords: Relugolix, Orgovyx; TAK-385; RVT-601 supplier, Estrogen Receptor, inhibitors

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