CAS No. 112568-12-4 Chemical Name: Antide Synonyms Antide Acetate; lyl-; ANTIDE; iturelix; Orf 23541; Brn 4866881; Antide impurity; ANTIDE (iturelix); Iturelix, ORF 23541; Antide >=97% (HPLC) CBNumber: CB7665086 Molecular Formula: C82H108ClN17O14 Molecular Weight: 1591.29 MDL Number: MFCD00133104 MOL File: 112568-12-4.mol
Last updated: 2026-01-21 16:49:52
Antide, is a GnRH and LH-RH antagonist, and with high anti-ovulatory and negligible histamine release activity.
Reversible inhibition of gonadotropin secretion and subsequent suppression of ovarian and testicular steroid secretio (gonadotropin releasing hormone antagonist).
Antide acetate was prepared as follows: the peptide intermediate was first treated with a suitable thiol to remove the Nps protecting group. It was then reacted with 2-benzyl-4-carboxypyridine in DMF in DCC as a coupling agent to acylate the Orn residue at the 5-position. After washing, the peptide resin was treated with piperidine to remove the Fmoc protecting group, followed by treatment with nicotinic acid and DIIC to acylate the D-Lys residue at the 6-position. Following cleavage and HPLC purification, the GnRH antagonist was tested and the peptide was considered effective in preventing ovulation in low-dose female mammals.
Antide (subcutaneously; 1, 3, 6, 10 and 15 mg/kg; once or on 5 consecutive days) can induce a long-term chemical castration in adult male rats and cynomolgus monkeys.
Animal Model: Cynomolgus monkey and rat Dosage: 1, 3, 6, 10 and 15 mg/kg Administration: Subcutaneous, once or on 5 consecutive days Result: Had a dose-dependent inhibitory effect on serum concentration of LH (only rat) and testosterone and on the weights of the testes, prostates and seminal vesicles. Achieved long-lasting castration-like effects at concentrations between 6 (less than or equal to 8 weeks) and 15 mg/kg (greater than 8 weeks) in the rat. Induced a prolonged inhibitory effect only at 15 mg/kg and the duration was only 2-3 weeks in the cynomolgus monkey.
Antide acetate (Ac-AA10-NH 2) is an LHRH antagonist and represses LH and FSH release from the pituitary gland. Antide Mw is 1590.6 Dalton.
