(D-Ser(tBu)6,AzaGly10)-LHRH acetate salt

Names

[ Name ]:
(D-Ser(tBu)6,AzaGly10)-LHRH acetate salt

[Synonym ]:
Goserelin acetate
Goserelin acetate [D-Ser(tBu)6,Azagly10]-LHRH acetate salt
Goserelin (acetate)

Biological Activity

[Description]:

Goserelin (ICI 118630) acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).IC50 value:Target: GnRH agonistGoserelin is used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty. It may also be used in the treatment of male-to-female transsexuals and is favoured above other anti-androgens in some countries, such as the UK. It is available as a 1-month depot and a long-acting 3-month depot. Goserelin stimulates the production of the sex hormones testosterone and estrogen in a non-pulsatile (non-physiological) manner.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GNRH Receptor

Research Areas >> Endocrinology

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
1695.5ºC at 760mmHg

[ Melting Point ]:
>190°C (dec.)

[ Molecular Formula ]:
C₆₁H₈₈N₁₈O₁₆

[ Molecular Weight ]:
1329.46

[ PSA ]:
493.39000

[ LogP ]:
-0.95

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.692

[ Storage condition ]:
−20°C

[ Water Solubility ]:
H2O: 20 mg/mL, clear, colorless

Safety Information

[ Symbol ]:

GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H360

[ Precautionary Statements ]:
P201-P280-P308 + P313

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
22-24/25

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
OK6369800

Articles

Stability of peptide drugs in the colon.

Eur. J. Pharm. Sci. 78 , 31-6, (2015)

This study was the first to investigate the colonic stability of 17 peptide molecules (insulin, calcitonin, glucagon, secretin, somatostatin, desmopressin, oxytocin, Arg-vasopressin, octreotide, ciclo...

Targeted gold nanoparticles enhance sensitization of prostate tumors to megavoltage radiation therapy in vivo.

Nanomedicine: Nanotechnology, Biology, and Medicine 11 , 1277-83, (2015)

We report potent radiosensitization of prostate cancers in vitro and in vivo using goserelin-conjugated gold nanorods. Progressive receptor-mediated internalization of conjugated nanorods over time in...

Toward oral delivery of biopharmaceuticals: an assessment of the gastrointestinal stability of 17 peptide drugs.

Mol. Pharm. 12(3) , 966-73, (2015)

A major barrier to successful oral delivery of peptide and protein molecules is their inherent instability in the lumen of the gastrointestinal tract. The aim of this study was to determine the stabil...