Naam:Leuprolide Acetate,Leuprorelin Acetate, Leuproreline Acetate, Leuprorelinum Acetate
Casnr:74381-53-6
Formule: C61H88N16O14
Moleculair:1269.45
Reeks: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
Zuiverheid:98%
Verschijning: wit poeder
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, uterine fibroids, 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. In aanvulling, 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. Bovendien, 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 may be used in the treatment of hormone-responsive cancers such as prostate cancer and breast cancer. It may also be used for estrogen-dependent conditions such as endometriosis or uterine fibroids.
2.It may be used for precocious puberty in both males and females, and to prevent premature ovulation in cycles of controlled ovarian stimulation for in vitro fertilization (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 |
SPECIFICATIE |
RESULTAAT |
| Verschijning |
Wit poeder |
Conformeert |
| Oplosbaarheid |
Soluble in water or 1% acetic acid at a
concentration of ≥1mg/ml to give a clear,
colorless solution |
Conformeert |
| 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 |
Conformeert
Conformeert
0.84
0.97
1.04
2.02
1.01
0.99
1.00
present |
| Specific Optical Rotation |
-38.0~-42.0° [A]20D(c=1,1% HAc) |
-39.2° |
| RelatedSubstance
(Door HPLC) |
Totaal onzuiverheden(%)≤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%
Conformeert
Conformeert
Conformeert
Conformeert
0.2% |
| Acetaat inhoud(Door HPLC) |
4.7~9.0% |
8.7% |
| Waterinhoud(Karel Fischer) |
≤5,0% |
1.4% |
| Sulfaat as |
≤0,3% |
Conformeert |
| Bacterial Endotoxins |
≤16.7 IU/mg |
Conformeert |
| Residual Organic Solvents |
Acetonitrile ≤0.041%(By GC)
DMF ≤0.088%(By GC)
MEOH ≤0.3%(By GC)
TFA ≤0.1%(Door HPLC) |
Conformeert
Conformeert
Conformeert
Conformeert |
| Analyse(Door watervrij, Azijnzuurvrij ) |
97.0~103,0% |
98.10% |
