Sufugolix

SKU: orb1304092

Description

Sufugolix (TAK-013) is an orally bioavailable, potent antagonist of the gonadotropin-releasing hormone (GnRH) receptor. It is utilized in preclinical research to investigate hormone-dependent conditions, with studies demonstrating its activity in both in vitro assays and in vivo models for potential therapeutic applications.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 308831-61-0
• MW: 667.72
• Purity: 95.06% (May vary between batches)
• Formula: C₃₆H₃₁F₂N₅O₄S
• SMILES: CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccccc3)c(=O)c2c1CN(C)Cc1ccccc1
• Target: LHRH,GNRH Receptor
• Solubility: DMSO:25 mg/mL (37.44 mM)

Bioactivity

• Target IC50:
  LHRH:0.1 nM.
• In Vivo:
  Oral administration of sufugolix at a 30 mg/kg dose causes almost complete suppression of plasma LH levels in castrated male cynomolgus monkeys for more than 24 hours. Sufugolix exhibits sufficient lipophilicity for enhanced membrane permeability and improved oral absorption in monkeys. Maximum plasma concentrations are 0.34 μM (6 hours post-administration) and 0.18 μM (4 hours post-administration) at 30 and 10 mg/kg doses, respectively.
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• In Vitro:
  Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. It effectively antagonizes LHRH function on CHO cells expressing the human (IC50=0.1 nM) and monkey (IC50=0.6 nM) receptors. High-temperature molecular dynamics calculation during the conformational analysis of sufugolix reveals that the cis conformer of the methoxyurea is more populated than the trans conformer.
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Storage & Handling

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

Alternative Names

Inhibitor, human LHRH, monkey LHRH, inhibit, TAK 013, TAK013, TAK-013, Sufugolix

Compound Identifiers

PubChem CID

3038517