Nombre:Acetato de leuprolida,Acetato de leuprorelina, Acetato de leuprorelina, Leuprorelinum Acetate
Cas No:74381-53-6
Fórmula: C61H88N16O14
Molecular:1269.45
Secuencia: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
Pureza:98%
Apariencia: polvo blanco
Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, fibromas uterinos, central precocious puberty and in vitro fertilization techniques. As its basic mechanism of action, leuprolide acetate suppresses gonadotrope secretion of luteinizing hormone and follicle-stimulating hormone that subsequently suppresses gonadal sex steroid production. Además, leuprolide acetate is presently being tested for the treatment of Alzheimer's disease, polycystic ovary syndrome, functional bowel disease, short stature, premenstrual syndrome and even as an alternative for contraception. Mounting evidence suggests that GnRH agonist suppression of serum gonadotropins may also be important in many of the clinical applications described above. Además, the presence of GnRHR in a multitude of non-reproductive tissues including the recent discovery of GnRHR expression in the hippocampi and cortex of the human brain indicates that GnRH analogs such as leuprolide acetate may also act directly via tissue GnRHRs to modulate (cerebro) function. De este modo, the molecular mechanisms underlying the therapeutic effect of GnRH analogs in the treatment of these diseases may be more complex than originally thought. These observations also suggest that the potential uses of GnRH analogs in the modulation of GnRH signaling and treatment of disease has yet to be fully realized.
1.La leuprorelina puede usarse en el tratamiento de cánceres que responden a hormonas, como el cáncer de próstata y el cáncer de mama.. También se puede utilizar para afecciones dependientes de estrógenos, como la endometriosis o los fibromas uterinos..
2.Puede usarse para la pubertad precoz tanto en hombres como en mujeres., y para prevenir la ovulación prematura en ciclos de estimulación ovárica controlada para fertilización in vitro (FIV).
3.Leuprore.lin, along with triptore, are often used to delay puberty in transgender youth until they are old enough to begin hormone replacement therapy. They are also sometimes used as superior alternatives to anti-androgens like spironolac.tone and cyproterone acetate for suppressing test osterone production in trans women.
| ELEMENTOS |
ESPECIFICACIÓN |
RESULTADO |
| Apariencia |
polvo blanco |
Cumple |
| Solubilidad |
Soluble en agua o 1% acetic acid at a
concentration of ≥1mg/ml to give a clear,
solución incolora |
Cumple |
| Identity |
A. Y
Same with the reference spectrum of Leuprolide
B. HPLC
Same with the reference solution
do. Amino Acid Analysis
Ser: Present
glu: 0.85~1.1
Pro: 0.85~1.1
leu: 1.80~2.2
tiro: 0.85~1.1
His: 0.85~1.1
Arg: 0.85~1.1
Trp: Present |
Cumple
Cumple
0.84
0.97
1.04
2.02
1.01
0.99
1.00
present |
| Rotación óptica específica |
-38.0~-42.0° [a]20D(c=1,1% HAc) |
-39.2° |
| RelatedSubstance
(Por HPLC) |
Impurezas totales(%)≤2,5%
acetyl-leuprolide≤1.0%
D-His-leuprolide≤0.5%
L-Leu6-leuprolide≤0.5%
D-Ser-leuprolide≤0.5%
Any other Impurity≤0.5% |
0.21%
Cumple
Cumple
Cumple
Cumple
0.2% |
| Contenido de acetato(Por HPLC) |
4.7~9.0% |
8.7% |
| Contenido de agua(Karl Fischer) |
≤5,0% |
1.4% |
| Sulphate ash |
≤0,3% |
Cumple |
| Endotoxinas bacterianas |
≤16.7 IU/mg |
Cumple |
| Residual Organic Solvents |
Acetonitrile ≤0.041%(By GC)
DMF ≤0.088%(By GC)
MEOH ≤0.3%(By GC)
TFA ≤0.1%(Por HPLC) |
Cumple
Cumple
Cumple
Cumple |
| Ensayo(Por anhidro, Sin ácido acético ) |
97.0~103,0% |
98.10% |
