Naam:Leuprolide-asetaat,Leuprorelin-asetaat, Leuproreline Acetate, Leuprorelinum Acetate
Cas No:74381-53-6
Formule: C61H88N16O14
Molekulêr:1269.45
Volgorde: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
Reinheid:98%
Voorkoms: wit poeier
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, endometriose, uteriene fibroïede, 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. Daarby, 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. Bowendien, 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 (brein) function. Dus, 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.Leuprorelin kan gebruik word in die behandeling van hormoon-responsiewe kankers soos prostaatkanker en borskanker. Dit kan ook gebruik word vir estrogeen-afhanklike toestande soos endometriose of uteriene fibroïede.
2.Dit kan gebruik word vir voorbarige puberteit by beide mans en vroue, en om voortydige ovulasie te voorkom in siklusse van beheerde ovariale stimulasie vir in vitro-bevrugting (IVF).
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.
| ITEMS |
SPESIFIKASIE |
RESULTAAT |
| Voorkoms |
Wit poeier |
Konformeer |
| Oplosbaarheid |
Oplosbaar in water of 1% acetic acid at a
concentration of ≥1mg/ml to give a clear,
colorless solution |
Konformeer |
| Identity |
A. EN
Same with the reference spectrum of Leuprolide
B. HPLC
Same with the reference solution
C. Amino Acid Analysis
Ser: Present
Glu: 0.85~1.1
Pro: 0.85~1.1
Leu: 1.80~2.2
Tyr: 0.85~1.1
His: 0.85~1.1
Arg: 0.85~1.1
Trp: Present |
Konformeer
Konformeer
0.84
0.97
1.04
2.02
1.01
0.99
1.00
present |
| Spesifieke optiese rotasie |
-38.0~-42.0° [a]20D(c=1,1% HAc) |
-39.2° |
| RelatedSubstance
(Deur HPLC) |
Total Impurities(%)≤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%
Konformeer
Konformeer
Konformeer
Konformeer
0.2% |
| Asetaat inhoud(Deur HPLC) |
4.7~9.0% |
8.7% |
| Waterinhoud(Karl Fischer) |
≤5,0% |
1.4% |
| Sulphate ash |
≤0.3% |
Konformeer |
| Bakteriese endotoksiene |
≤16.7 IU/mg |
Konformeer |
| Residual Organic Solvents |
Acetonitrile ≤0.041%(By GC)
DMF ≤0.088%(By GC)
MEOH ≤0.3%(By GC)
TFA ≤0.1%(Deur HPLC) |
Konformeer
Konformeer
Konformeer
Konformeer |
| Assay(Deur Anhydrous, Asynsuurvry ) |
97.0~103.0% |
98.10% |