Abarelix

SKU: orb1310028

Description

Abarelix (PPI 149) is a synthetic GnRH antagonist used in research for prostate cancer. It directly inhibits gonadotropin release, providing a rapid chemical castration effect. Its mechanism has been validated in both in vitro receptor binding assays and in vivo animal models of hormone-dependent cancers.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 183552-38-7
• MW: 1416.06
• Purity: >99.99% (May vary between batches)
• Formula: C₇₂H₉₅ClN₁₄O₁₄
• SMILES: CC(C)C[C@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O
• Target: GNRH Receptor
• Solubility: DMSO:14.2 mg/mL (10.03 mM)

Bioactivity

• In Vitro:
  Abarelix, at concentrations of 30 and 300 µg/mL, significantly increases histamine release. It rapidly and considerably lowers follicle-stimulating hormone levels below those achieved by LHRH agonists. As the inaugural GnRH antagonist developed, Abarelix achieves fast and sustained testosterone reductions to castrate levels without requiring concurrent antiandrogen therapy, exhibiting a remarkably low short-term complication rate. Unlike other treatments, it avoids the testosterone surge that can exacerbate symptoms or disease progression, particularly in patients with metastatic, symptomatic conditions, facilitating quicker medical castration.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Abarelix, GnRHR, GNRHReceptor, GNRH Receptor, GnRH Receptor, GNRHR, Gonadotropin releasing hormone receptor, Inhibitor, inhibit, R-3827, R3827, PPI149, PPI-149, PPI 149, R 3827

Compound Identifiers

PubChem CID

16131215