名前:Leuprolide Acetate,Leuprorelin Acetate, Leuproreline Acetate, Leuprorelinum Acetate
カス番号:74381-53-6
方式: C61H88N16O14
分子:1269.45
順序: Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt
純度:98%
外観: 白い粉
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, 子宮内膜症, 子宮筋腫, 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 addition, 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. Moreover, 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 (脳) function. したがって, 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 |
SPECIFICATION |
RESULT |
| 外観 |
白い粉 |
適合 |
| 溶解性 |
Soluble in water or 1% acetic acid at a
concentration of ≥1mg/ml to give a clear,
colorless solution |
適合 |
| Identity |
あ. IR
Same with the reference spectrum of Leuprolide
B. HPLC
Same with the reference solution
ハ. Amino Acid Analysis
することが: 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 |
適合
適合
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
(By 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%
適合
適合
適合
適合
0.2% |
| アセテート含有量(By HPLC) |
4.7~9.0% |
8.7% |
| 含水量(カール・フィッシャー) |
≤5.0% |
1.4% |
| Sulphate ash |
≤0.3% |
適合 |
| 細菌エンドトキシン |
≤16.7 IU/mg |
適合 |
| Residual Organic Solvents |
Acetonitrile ≤0.041%(By GC)
DMF ≤0.088%(By GC)
MEOH ≤0.3%(By GC)
TFA ≤0.1%(By HPLC) |
適合
適合
適合
適合 |
| アッセイ(無水による, 無酢酸 ) |
97.0~103.0% |
98.10% |
