Deslorelin 57773-65-6

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Deslorelin

Deslorelin acetate is an injectable gonadotropin releasing hormone super-agonist also known as an LHRH agonist. It stops the production of sex hormones . Deslorelin Acetate is marketed by Peptech with the brand name Ovuplant. It is currently approved for use in veterinary medicine and is used to induce ovulation in mares as part of the artificial insemination process. It is also used to stabilize high-risk pregnancies, mainly of livestock. Unlike other GnRH agonists, which are mainly used to inhibit luteinizing hormone and follicle-stimulating hormone by their ultimate downregulation of the pituitary gland, Deslorelin is primarily used for the initial flare effect upon the pituitary, and its associated surge of LH secretion.

Pharmacokinetics

Deslorelin is a synthetic analogue of a naturally occurring luteinising-hormone releasing hormone . Bioavailability is almost complete.

Clinical trials

Deslorelin was successfully trialed in the US and was approved for veterinary use under certain circumstances. In Europe, it was approved for use in equine assisted reproduction. . It is also being trialed in humans to study its efficacy in treatment of breast cancer in women, and in treating precocious puberty and congenital adrenal hyperplasia in male and female children. As of early 2009, this drug is not approved for use in the US, other than within approved clinical trials.

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Systematic (IUPAC) name: (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
Deslorelin CAS number: 57773-65-6
ATC code: H01CA93
PubChem: 7979044
DrugBank:
Formula: C64H83N17O12
Molecular mass: 1282.45 g/mol
Deslorelin Assay/Purity: Typically NLT 98%
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