Bioactivity | Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment. | ||||||
Invitro | Abarelix (30 and 300 µg/mL) causes significantly increased histamine release[1]. Abarelix is the firstGnRH antagonist to be developed, and can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term[2]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix does not cause a surge in serum testosterone that can precipitate a flare phenomenon or worsening of disease, particularly dangerous for patients with metastatic, symptomatic disease, and produces medical castration more quickly[3]. | ||||||
Name | Abarelix | ||||||
CAS | 183552-38-7 | ||||||
Shortening | Ac-{d-2-Nal}-{d-4-Cpa}-{d-3-Pal}-S-{NMyr}-{d-Asp}-L-K(ipr)-P-{d-Ala}-NH2 | ||||||
Formula | C72H95ClN14O14 | ||||||
Molar Mass | 1416.06 | ||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||
Storage | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |