Leuprorelin Acetate (CAS 74381-53-6) is a synthetic GnRH (gonadotropin-releasing hormone) agonist nonapeptide of the LHRH decapeptide analogue chemical class. Its sequence is pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt. It has D-Leu6 and a C-terminal ethylamide (Pro9-NHEt) instead of the native Gly10-NH2, which makes it more than 100 times more potent and resistant to enzymatic degradation. Leuprorelin is FDA-approved for prostate cancer, endometriosis, uterine leiomyomata, and central precocious puberty. It works in a strange way: when taken for a long time, it lowers the levels of GnRH receptors in the pituitary gland, which lowers LH/FSH and testosterone/estradiol to levels that are not enough to cause puberty. Process-related impurities consist of sequence deletion peptides (des-His2, des-Trp3, des-Ser4), amino acid substitution analogues, oxidized methionine-containing scrambled sequences, and D-amino acid epimers. ICH Q6B sets the rules for characterizing biological and peptide APIs.
ApiSyn sells Leuprorelin Acetate and other peptide sequence deletion impurity standards that can be used to check the quality of GnRH peptides and validate the RP-HPLC method.
| Chemical Name | (5-Oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-leucyl-l-leucyl-l-arginyl-N-ethyl-l-prolinamide acetate (salt)) |
| Molecular Formula | C59H84N16O12 : C2H4O2 |
| Molecular Weight | 1209.4 : 60.1 |
| CAS Number | 74381-53-6 |