Relugolix

SKU: orb1303979

Description

Relugolix is an oral GnRH receptor antagonist that suppresses LH and FSH release, leading to reduced testosterone production. This mechanism is applied in research for hormone-dependent cancers like prostate cancer, utilizing both in vitro receptor binding assays and in vivo xenograft models to study its antineoplastic effects.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 737789-87-6
• MW: 623.63
• Purity: 98.64% (May vary between batches)
• Formula: C₂₉H₂₇F₂N₇O₅S
• SMILES: CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccc(OC)nn3)c(=O)c2c1CN(C)C
• Target: GNRH Receptor
• Solubility: DMSO:250 mg/mL (400.88 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (1.6 mM)

Bioactivity

• Target IC50:
  TNK2 (D163E mutations):38nM|TNK2 (R806Q mutations):113 nM

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

antagonistic, Inhibitor, GnRH Receptor, GnRH, GNRHR, GnRHR, GNRH Receptor, GNRHReceptor, Gonadotropin releasing hormone receptor, FSH, endometriosis, inhibit, prostate cancer, TAK 385, TAK385, TAK-385, RVT 601, RVT601, RVT-601, Relugolix, uterine fibroid

Compound Identifiers

PubChem CID

10348973