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Leuprorelin

CAS No.
53714-56-0
Chemical Name:
Leuprorelin
Synonyms
LEUPROLIDE;Lucrin;Leuplin;a-43818;Carcinil;Enantone;nghormone;LEUPRORELIN;LEUPROPELIN;Leuprorelinum
CBNumber:
CB8398455
Molecular Formula:
C59H84N16O12
Molecular Weight:
1209.4
MDL Number:
MFCD00167544
MOL File:
53714-56-0.mol
TDS File:
TDS
Last updated:2026-08-04 11:17:55

Leuprorelin Properties

alpha D25 -31.7° (c = 1 in 1% acetic acid)
Density 1.44±0.1 g/cm3(Predicted)
storage temp. −20°C
solubility DMSO (Slightly), Methanol (Slightly), Water (Slightly)
pka 9.82±0.15(Predicted)
Water Solubility Soluble in water at 1mg/ml
Stability Hygroscopic
InChIKey RGLRXNKKBLIBQS-VAZQWRJQNA-N
CAS DataBase Reference 53714-56-0(CAS DataBase Reference)
FDA UNII EFY6W0M8TG
ATC code L02AE02

SAFETY

Risk and Safety Statements

Symbol(GHS)  Health Hazard (GHS08)
GHS08
Signal word  Danger
Hazard statements  H360
Precautionary statements  P201-P280-P308+P313
Safety Statements  22-24/25
WGK Germany  2
RTECS  OH6390000
Hazardous Substances Data 53714-56-0(Hazardous Substances Data)

Leuprorelin price More Price(24)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich L0376000 Leuprorelin European Pharmacopoeia (EP) Reference Standard 53714-56-0 1 mg $254 2026-04-30 Buy
Sigma-Aldrich L0376000 Leuprorelin European Pharmacopoeia (EP) Reference Standard 53714-56-0 l0376000 $220 2024-03-01 Buy
Biorbyt Ltd orb1089659 Leuprorelin >98% 53714-56-0 100mg $210 2026-05-06 Buy
Biorbyt Ltd orb1089659 Leuprorelin >98% 53714-56-0 250mg $330 2026-05-06 Buy
Biorbyt Ltd orb1089659 Leuprorelin >98% 53714-56-0 1g $640 2026-05-06 Buy
Product number Packaging Price Buy
L0376000 1 mg $254 Buy
L0376000 l0376000 $220 Buy
orb1089659 100mg $210 Buy
orb1089659 250mg $330 Buy
orb1089659 1g $640 Buy

Leuprorelin Chemical Properties,Uses,Production

Description

Leuprorelin(Leuprolide ) is a synthetic water-soluble nonapeptide with both ends closed, and also a highly active analogue of luteinizing hormone releasing hormone (LHRH or GnRH) produced by the hypothalamus. It can stimulate the pituitary gland to secrete gonadotropins and induce the production of steroids in the reproductive organs. 

Mechanism of action

Leuprorelin is a nonapeptide synthetic analogue of Luteinizing Hormone Releasing Hormone (LHRH), which can promote the release of follicle stimulating hormone from the anterior pituitary, thereby reducing the increased testosterone concentration to castrate levels. When the administration is stopped, gonadotropins and androgens can return to normal concentrations.

Uses

Leuprorelin is a nonapeptide synthetic analogue of gonadotropin (GnRH), which can promote the release of luteinizing hormone (LHRH) and follicle stimulating hormone (FSH) from the anterior pituitary, regulate the secretion of gonadal hormones, and increase the serum levels of testosterone and dihydrotestosterone. Concentration, so as to achieve the function of treating reproductive system diseases. It is used to treat prostate cancer, uterine fibroids, ovarian cysts, breast cancer and cryptorchidism in children.

Pharmacokinetics

Leuprolide acetate(Leuprorelin) is ineffective orally. Good absorption by subcutaneous or intramuscular injection. A single subcutaneous injection of 3.75mg, the blood concentration of 1 to 2 days peaked at 1 to 2ng/ml. For prostate cancer, 3.75mg is injected subcutaneously each time, once every 4 Chemicalbook weeks, for a total of 3 injections, reaching a steady-state blood concentration of 0.1-1ng/ml. This product is hydrolyzed into 4 degradation products in the body and excreted by the kidneys. The urinary excretion rates of the original drug and metabolites were 2.9% and 1.5% after a single subcutaneous injection 28 days.

Adverse reactions

The main side effects of Leuprorelin are fever, heat sensation and elevated AST, ALT, γ-GTP and AKP. Sometimes there are facial flushing, sweating, loss of libido, impotence, feminized breasts, testicular atrophy, perineal discomfort and other endocrine system phenomena; abnormal electrocardiogram and increased ratio of heart and chest, bone pain, shoulder, lower back, limb pain, Urinary retention, frequent urination, hematuria, nausea, vomiting, loss of appetite, rash, itching and other allergic reactions and pain, induration, and redness at the injection site. Rarely, edema, chest pressure, chills, tiredness, weight gain, abnormal perception, tinnitus, hearing loss, TG, uric acid and BUN are increased.

Chemical Properties

Hygroscopic, white or almost white powder.

Originator

Eligard,Atrix Laboratories, Inc.

Uses

Highly active luteinizing hormone releasing hormone (LHRH) agonist

Uses

Gonadotropin releasing hormone (gonadorelin) analogue; treatment of prostate cancer.

Definition

ChEBI: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. Leuprorelin is a synthetic nonapeptide analogue of gonadotropin-releasi g hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.

Indications

Leuprolide is a potent LH-RH agonist for the first several days to a few weeks after initiation of therapy, and therefore, it initially stimulates testicular and ovarian steroidogenesis. Because of this initial stimulation of testosterone production, it is recommended that patients with prostatic cancer be treated concurrently with leuprolide and the antiandrogen flutamide (discussed earlier). Leuprolide is generally well tolerated, with hot flashes being the most common side effect.

Therapeutic Function

Antineoplastic

Synthesis

The synthesis process of Leuprorelin includes the following steps:
(1) Fmoc-Pro-HMPB-AM resin is obtained from Fmoc-Pro-OH and HMPB-AM resin with a substitution degree of 0.2mmol/g~1.2mmol/g as starting materials;
(2) The Fmoc-Pro-HMPB-AM resin was coupled one by one by Fmoc/tBu solid phase method to connect amino acids with protective groups in sequence, and the side chain fully protected leuprolide precursor peptide-HMPB-AM was synthesized Resin;
(3) Cut the side chain fully protected leuprolide precursor peptide-HMPB-AM resin to obtain the side chain fully protected leuprolide precursor peptide;
(4) Fully protected side chain leuprolide precursor peptide undergoes ethylamination to obtain side chain fully protected leuprolide;
(5) Leuprolide is fully protected on the side chain by removing the side chain protecting group to obtain the crude leuprolide peptide;
(6) The crude leuprorelin peptide is separated and purified by a high-pressure liquid phase column and lyophilized to obtain the leuprolide refined peptide.

914200-76-3
53714-56-0
Synthesis of Leuprorelin from 1-9-Luteinizing hormone-releasing factor (swine), 2-[1-(triphenylmethyl)-L-histidine]-4-[O-(1,1-dimethylethyl)-L-serine]-5-[O-(1,1-dimethylethyl)-L-tyrosine]-6-D-leucine-8-[N5-[[[(2,3-dihydro-2,2,4,6,7-pentamethyl-5-benzofuranyl)sulfonyl]amino]iminomethyl]-L-ornithine]-9-(N-ethyl-L-prolinamide)-
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View Lastest Price from Leuprorelin manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Leuprorelin pictures 2026-09-10 Leuprorelin
53714-56-0
$1000.00 1g >=99% (HPLC), USP43 10000000 Chengdu Shengnuo Biopharm Co.,Ltd
Leuprorelin pictures 2026-05-28 Leuprorelin
53714-56-0
$1.90 1KG 99% 10 ton Hebei Chuanghai Biotechnology Co,.LTD
Leuprorelin pictures 2026-03-20 Leuprorelin
53714-56-0
$1.00 1KG 99% 10 mt Hebei Chuanghai Biotechnology Co., Ltd
  • Leuprorelin pictures
  • Leuprorelin
    53714-56-0
  • $1000.00
  • >=99% (HPLC), USP43
  • Chengdu Shengnuo Biopharm Co.,Ltd
  • Leuprorelin pictures
  • Leuprorelin
    53714-56-0
  • $1.90
  • 99%
  • Hebei Chuanghai Biotechnology Co,.LTD
  • Leuprorelin pictures
  • Leuprorelin
    53714-56-0
  • $1.00
  • 99%
  • Hebei Chuanghai Biotechnology Co., Ltd
LH-RH LEUPROLIDE LEUPROLIDE (HUMAN) LEUPRORELIN [DES-GLY10, D-LEU6, PRO-NHET9]-LUTEINIZING HORMONE-RELEASING HORMONE HUMAN (DES-GLY10,D-LEU6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING HORMONE (DES-GLY10,D-LEU6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING FACTOR [DES-GLY10, D-LEU6, PRO-NHET9]-LH-RH (HUMAN) DES-GLY10,[P-LEU6]-LH-RH ETHYLAMIDE (DES-GLY10,D-LEU6,PRO-NHET9)-LHRH (DES-GLY10,D-LEU6,PRO-NHET9)-GONADOTROPIN-RELEASING HORMONE [DES-GLY10, DLEU 6, PRONHET9] [DES-GLY10, DLEU6, PRO9]-LUTEINIZING HORMONE-RELEASING HORMONE, ETHYL AMIDE [DES-GLY10, DLEU6, PRO9]-LH-RH, ETHYL AMIDE GLP-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO-NHET 5-OXOPRO-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO-NHC2H5 PGLU-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO-NHET PGLU-HIS-TRP-SER-TYR-P-LEU-LEU-ARG-PRO-NHET PYROGLU-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO NHCH2CH3 PYR-HIS-TRP-SER-TYR-D-LEU-LEU-ARG-PRO-NHET N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1-[2-(ethylcarbamoyl)-1-pyrrolidinyl]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(4-h 6-D-Leucine-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing factor(pig) Carcinil Enantone Leuplin Lucrin (D-Leu6, des-Gly-NH210)-LH-RH ethylamide Des-Gly10-[D-Leu6]-LH-releasing hormone ethylamide N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(Diaminomethylideneamino)-1-[2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxo-pentan-2-yl]carbamoyl]-3-methyl-butyl]carbamoyl]-3-methyl-butyl]carbamoyl]-2-(4-hydroxyphenyl)ethyl]carbamoyl]-2-hydroxy-ethyl]carbamoyl]-2-(1H-indol-3-yl)ethyl]carbamoyl]-2-(3H-imidazol-4-yl)ethyl]-5-oxo-pyrrolidine-2-carboxamide [D-Leu6,des-Gly10]GnRH ethylamide 10-des-Gly-6-D-Leu-LH-RH-ethylamide 5-Oxo-L-Pro-L-His-L-Trp-L-Ser-L-Tyr-D-Leu-L-Leu-L-Arg-L-Pro-N-ethyl-NH2 GLP-HIS-TRP-SER-TYR-DLEU-LEU-ARG-PRO-NHET: GLP-HWSY-DL-LRP-NHET 1-9-LUTEINIZING HORMONE-RELEASING FACTOR (SWINE), 6-D-LEUCINE-9-(N-ETHYL-L-PROLINAMIDE)- LEUPROLIDE ACETATE PH. EUR. Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt acetate salt Leuprorelin Acetate(Leuprolide Acetate) Leuprolide, Leuprorelin, Leuproreline, Leuprorelinum Leuprorelinum LEUPRORELIN (LEUPROLIDE) ACETATE Leuprorelin###Leuprorelin acetate 1-(2-cyclohexyl-1-methylethyl)hydrazine hydrochloride Leuprelin Acetate (d-leu(sup6),des-gly-nh2(sup10),pro-ethylamide(sup9))-gnrh (d-leu(sup6),des-gly-nh2(sup10),pro-ethylamide(sup9))-gonadotropin-releasi (d-leu(sup6),des-gly-nh2(sup10),pro-ethylamide(sup9))-lhrh a-43818 de)-10-deglycinamide- luteinizinghormone-releasinghormone(pig),6-d-leucine-9-(n-ethyl-l-prolinami nghormone 5-Oxo-L-prolil-L-histidil-L-tryptophil-L-seril-L-thyrozil-D-leucil-L-arginil-N-ethyl-L-prolinamide LEUPROPELIN Leuprorelin mesylate Leuprorelin Acetate / Leuprorelin Leuprorelin CRS Leuprorelin USP/EP/BP Anti-cancer Leuprorelin acetate Leuprorelin (L0376000) Leuprolide Acetate(net)