Leuprolide Acetate

Catalog No.S3718 Synonyms: Leuprorelin Acetate

For research use only.

Leuprolide acetate (Leuprorelin) 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, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques.

Leuprolide Acetate Chemical Structure

CAS No. 74381-53-6

Selleck's Leuprolide Acetate has been cited by 1 Publication

Purity & Quality Control

Choose Selective GNRH Receptor Inhibitors

Biological Activity

Description Leuprolide acetate (Leuprorelin) 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, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques.
Targets
GnRHR [1]
In vitro

Leuprolide acetate is a synthetic nonapeptide that is a potent gonadotropin-releasing hormone receptor (GnRHR) agonist. Leuprolide acetate suppresses gonadotrope secretion of luteinizing hormone and follicle-stimulating hormone that subsequently suppresses gonadal sex steroid production[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO NECwVI5HfW6ldHnvckBie3OjeR?= M3vie2lvcGmkaYTpc44hd2ZiW{GyOWledGW3cILvdoVtcW5iYnnu[Ilv\yC2bzDoeY1idiC{ZXPvcYJqdmGwdDDMTHJJKHKnY3XweI9zKGW6cILld5Nm\CCrbjDDTG8h[2WubIOsJGlEPTBiPTCwMlMhdk1w M4\mOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4N{i5O|M5Lz5zNke4PVc{QDxxYU6=
HEK293 NFfHWVZHfW6ldHnvckBie3OjeR?= MlnRSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZS2WeYK2MEBJcXN3IH\yc40hcHWvYX6gUGhTUDFicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUyB{OUOgZ4VtdHNiYX\0[ZIhOTZidH:gNVkhcHK|IHL5JIdidW2jIHPveY51\XJuIFnDOVAhRSByLke2JI5ONg>? MknHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzMke5PFcoRjJ|MUK3PVg4RC:jPh?=
Assay
Methods Test Index PMID
Western blot PCNA / Bcl-2 / B-actin ; Cleaved caspase3 / GAPDH ; GRP78 / GAPDH ; SOD1 / CAT 24516352 25367189 29062464
Growth inhibition assay Cell Viability 24516352
IHC Klüver-Barrera Stain ; Masson's trichrome staining 26807118 27189011
Immunofluorescence RYR1 ; Cortex / medulla ; TUNEL 29062464 19380833 25367189
IHC & Immunofluorescence PAR / PARP-1 28851861
In vivo Leuprolide acetate is used for diverse clinical applications, including the treatment of prostate cancer, endometriosis, uterine fibroids, central precocious puberty and in vitro fertilization techniques. 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. Leuprolide acetate is considered to be a very safe and tolerable drug[1].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: PC-3 cells
  • Concentrations: 10−6 M or 10−11 M
  • Incubation Time: 6, 12, 18, 24 and 30 days.
  • Method:

    The cells were seeded at a density of 25,000 cells/ml of standard culture medium in 40-mm TPP dishes. Once they adhered to the culture plates (after 24 h), the medium was renewed with DMEM supplemented with 5% charcoal-treated FBS (CH-FBS) and 10−6 M or 10−11 M Leuprolide acetate. The medium was changed every 48 h, while LA was added daily to the cultures. PC-3 cells were exposed to the analogue for 6, 12, 18, 24 and 30 days. Every six days, cells were trypsinized, seeded (25,000 cells/ml) into the 40-mm TPP dishes and, once they adhered to the culture plates, treated as described above for a further 6-day period. At the end of each treatment period, the cells were analyzed by AFM. In all the experiments, control cultures were run in parallel.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 1269.45
Formula

C59H84N16O12. C2H4O2

CAS No. 74381-53-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N6.CC(=O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02920359 Completed Drug: LEUPRORELIN ACETATE There Are no Conditions Under Study. Healthy Volunteers Parc de Salut Mar November 17 2016 Phase 1
NCT01960881 Completed -- Prostate Cancer AbbVie|JSS Medical Research; CMX Research Inc.; Canadian Urology Research Consortium September 19 2013 --
NCT01442246 Active not recruiting Drug: Leuprorelin Acetate Metastases UNICANCER|Astellas Pharma Inc July 2011 Phase 3
NCT01069094 Completed Drug: Progenta|Drug: Lucron Depot|Drug: Placebo Uterine Leiomyomata Repros Therapeutics Inc. July 2004 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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Handling Instructions

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