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65807-02-5

65807-02-5 structure
65807-02-5 structure
  • Name: Goserelin
  • Chemical Name: Goserelin
  • CAS Number: 65807-02-5
  • Molecular Formula: C59H84N18O14
  • Molecular Weight: 1269.41
  • Catalog: API Hormone and endocrine-regulating drugs Gonadotropin
  • Create Date: 2018-02-05 08:00:00
  • Modify Date: 2024-01-02 20:01:33
  • Goserelin(ICI 118630) 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.

Name Goserelin
Synonyms (2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name)
5-Oxo-L-prolyl-L-histidyl-N-[(1S,4S,7R,10S,13S)-18-amino-13-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]-1-pyrrolidinyl}carbonyl)-4-(4-hydroxybenzyl)-1-(hydroxymethyl)-18-imino-10-isobutyl-7-{[(2-methyl-2-propanyl)oxy]methyl}-2,5,8,11-tetraoxo-3,6,9,12,17-pentaazaoctadec-1-yl]-L-tryptophanamide
(2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-13-[(1,1-diméthyléthoxy)méthyl]-10-(4-hydroxybenzyl)-7-(hydroxyméthyl)-1-(1H-imidazol-
2-Pyrrolidinecarboxylic acid, 1-[(2S,5S,8R,11S,14S,17S,20S)-2-[3-[(aminoiminomethyl)amino]propyl]-8-[(1,1-dimethylethoxy)methyl]-14-(hydroxymethyl)-11-[(4-hydroxyphenyl)methyl]-20-(1H-imidazol-4-ylmethyl)-17-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-1,4,7,10,13,16,19,22-octaoxo-22-[(2S)-5-oxo-2-pyrrolidinyl]-3,6,9,12,15,18,21-heptaazadocos-1-yl]-, 2-(aminocarbonyl)hydrazide, (2S)-
(2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-13-[(1,1-diméthyléthoxy)méthyl]-10-(4-hydroxybenzyl)-7-(hydroxyméthyl)-1-(1H-imidazol-4-ylméthyl)-24-imino-4-(1H-indol-3-ylméthyl)-16-(2-méthylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatétracos-1-yl]-5-oxopyrrolidine-2-carboxamide
(2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidine-2-carboxamide
Decapeptide I
(2S)-N-[(1S,4S,7S,10S,13R,16S,19S)-24-Amino-13-(tert-butoxymethyl)-19-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-10-(4-hydroxybenzyl)-7-(hydroxymethyl)-1-(1H-imidazol-4-ylmethyl)-24-imino-4-(1H-indol-3-ylmethyl)-16-(2-methylpropyl)-2,5,8,11,14,17-hexaoxo-3,6,9,12,15,18,23-heptaazatetracos-1-yl]-5-oxopyrrolidin-2-carboxamid
1-(5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-O-tert-butyl-D-seryl-L-leucyl-L-arginyl-L-prolyl)semicarbazide
(2S)-N-[(2S,5S,8S,11S,14R,17S,20S)-25-amino-14-(tert-butoxymethyl)-20-({(2S)-2-[(2-carbamoylhydrazinyl)carbonyl]pyrrolidin-1-yl}carbonyl)-11-(4-hydroxybenzyl)-8-(hydroxymethyl)-1-(1H-imidazol-4-yl)-25-imino-5-(1H-indol-3-ylmethyl)-17-(2-methylpropyl)-3,6,9,12,15,18-hexaoxo-4,7,10,13,16,19,24-heptaazapentacosan-2-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name)
Goserelin
(2S)-N-[(2S,5S,8S,11S,14R,17S,20S)-25-Amino-14-(tert-butoxymethyl)-20-({(2S)-2-[(2-carbamoylhydrazino)carbonyl]pyrrolidin-1-yl}carbonyl)-11-(4-hydroxybenzyl)-8-(hydroxymethyl)-1-(1H-imidazol-4-yl)-25-imino-5-(1H-indol-3-ylmethyl)-17-isobutyl-3,6,9,12,15,18-hexaoxo-4,7,10,13,16,19,24-heptaazapentacosan-2-yl]-5-oxopyrrolidine-2-carboxamide (non-preferred name)
Description Goserelin(ICI 118630) 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
References

[1]. Goserelin, From Wikipedia

Density 1.5±0.1 g/cm3
Molecular Formula C59H84N18O14
Molecular Weight 1269.41
PSA 493.39000
LogP -0.95
Index of Refraction 1.692
Storage condition −20°C
Water Solubility H2O: 20 mg/mL, clear, colorless

CHEMICAL IDENTIFICATION

RTECS NUMBER :
OK6369800
CHEMICAL NAME :
Luteinizing hormone-releasing factor (pig), 6-(O-1,1-dimethylethyl)-D-serene)-10- deglycinamide-, 2-(aminocarbonyl)hydrazide
CAS REGISTRY NUMBER :
65807-02-5
LAST UPDATED :
199510
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C59-H84-N18-O14
MOLECULAR WEIGHT :
1269.61

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
51 ug/kg
TOXIC EFFECTS :
Brain and Coverings - changes in circulation (hemorrhage, thrombosis, etc.) Sense Organs and Special Senses (Eye) - diplopia Nutritional and Gross Metabolic - other changes
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 345,458,1995 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
12 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands
REFERENCE :
JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 10,478,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
12 mg/kg
SEX/DURATION :
male 1 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - other effects on male Endocrine - androgenic
REFERENCE :
JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 10,478,1989
Safety Phrases S22-S24/25
WGK Germany 3