Name | Leuprolide acetate |
Synonyms | lupron tap-144 Procrin Prostap Abbott 43818 Procren Depot Leuprolide acetate Leuprorelin Acetate leutenizinghormone-releasingfactor(pig),6-d-leucine-9-(n-ethyl-l-prolinamid 6-D-Leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing Hormone-Releasing Factor Acetate(Pig) 5-Oxo-L-prolil-L-histidil-L-tryptophil-L-seril-L-thyrozil-D-leucil-L-arginil-N-ethyl-L-prolinamide acetate |
CAS | 74381-53-6 |
EINECS | 686-285-8 |
InChI | InChI=1/C59H84N16O12.C2H4O2/c1-6-63-57(86)48-14-10-22-75(48)58(87)41(13-9-21-64-59(60)61)68-51(80)42(23-32(2)3)69-52(81)43(24-33(4)5)70-53(82)44(25-34-15-17-37(77)18-16-34)71-56(85)47(30-76)74-54(83)45(26-35-28-65-39-12-8-7-11-38(35)39)72-55(84)46(27-36-29-62-31-66-36)73-50(79)40-19-20-49(78)67-40;1-2(3)4/h7-8,11-12,15-18,28-29,31-33,40-48,65,76-77H,6,9-10,13-14,19-27,30H2,1-5H3,(H,62,66)(H,63,86)(H,67,78)(H,68,80)(H,69,81)(H,70,82)(H,71,85)(H,72,84)(H,73,79)(H,74,83)(H4,60,61,64);1H3,(H,3,4)/t40-,41-,42-,43+,44-,45-,46-,47-,48-;/m0./s1 |
InChIKey | RGLRXNKKBLIBQS-XNHQSDQCSA-N |
Molecular Formula | C61H88N16O14 |
Molar Mass | 1269.47 |
Melting Point | 150-155°C |
Boling Point | 1720.5°C at 760 mmHg |
Flash Point | 994.3°C |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Vapor Presure | 0mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
Merck | 14,5457 |
Storage Condition | -20°C |
Use | Endometriosis and precocious puberty |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 2 |
RTECS | OH6390000 |
HS Code | 29371900 |
Use | leuprolide acetate is a synthetic rh class non-peptide agonist. Antineoplastic drugs (hormones). |
properties | Leuprorelin acetate (Leuprorelin/leuprolide acetate,LA) is a synthetic water-soluble nonapeptide, its amino acid sequence is 5-oxo-l-prolyl-L-group Aminoacyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide monoacetate, molecular weight of 1269.47, soluble in water, ethanol and propylene glycol, pka6.9. |
Anti-cancer drugs | Leuprorelin acetate is a kind of hormone commonly used anti-cancer drugs, the acetate salt of leuprorelin, a nonpeptide synthetic analog of gonadotropin-releasing hormone (LHRH, a decapeptide), which is a LH-RH antagonist produced by the hypothalamus, it stimulates the anterior pituitary to release gonadotropins and follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This product is similar to the structure of LHRH, the role of the anterior pituitary also has to promote the release of FSH, LH function, thereby increasing the serum concentration of testosterone and dihydrotestosterone. Clinically for the maintenance treatment of advanced prostate cancer, but in the application of this product after about 1 week, the number of active receptors will be reduced, the secretion of gonadotropin will also be reduced. After 2 to 4 weeks, the concentration of testosterone and dihydrotestosterone can be reduced to the level of castration. When discontinued, gonadotropins and androgens can rise to normal concentrations. it should be noted that this product is ineffective by oral administration and absorbed well by subcutaneous or intramuscular injection. T1/2 for parenteral administration is 3 h. No accumulation in the body, the drug and metabolites in the urine excretion rates were 2.9% and 1.5%. Ethanol can strengthen the role of this product, the treatment process should not drink, so as not to control the occurrence of adverse reactions. In the first week of treatment should be as much as possible to hospital for monitoring, select experienced physicians to guide medication, in order to prevent serious neurological complications, urethral obstruction. The injection site should be changed frequently. |
adverse reactions | worsening bone pain, hematuria, urethral obstruction, temporary symptoms such as lower limb Fatigue can be improved after continuing treatment for 1 to 2 weeks. Also visible paroxysmal Fever, vertigo, visual impairment, depression, Nausea, Vomit, Diarrhea, palpitations, night sweats, hair loss, impotence, decreased libido, local injection may appear mild transient erythema, tingling, itching, swelling and induration. |
biological activity | Leuprolide acetate (Leuprorelin) is a synthetic nonapeptide, for a variety of clinical treatments, including prostate cancer, endometriosis, uterine leiomyoma, central precocious puberty and in vitro fertilization. |
Target | Value |