Relugolix

Catalog No.S5808 Batch:S580801

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Technical Data

Formula

C29H27F2N7O5S
Molecular Weight 623.63 CAS No. 737789-87-6
Solubility (25°C)* In vitro DMSO 61 mg/mL (97.81 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.
Targets
monkey GnRHR [2]
(Cell-free assay)		 human GnRHR [2]
(Cell-free assay)
0.32 nM 0.33 nM
In vitro 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)[2].
In vivo 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[2].

Protocol (from reference)

Animal Study:

[2]
  • Animal Models

    Six-week-old male hGNRHR-knock-in mice

  • Dosages

    3, 10 or 30 mg/kg

  • Administration

    oral

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.