CAS 76712-82-8|Histrelin

Introduction：Basic information about CAS 76712-82-8|Histrelin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Histrelin BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles42
8. Synonyms

Common Name	Histrelin
CAS Number	76712-82-8	Molecular Weight	1323.502
Density	1.5±0.1 g/cm3	Boiling Point	1800.6ºC at 760 mmHg
Molecular Formula	C₆₆H₈₆N₁₈O₁₂	Melting Point	/
MSDS	ChineseUSA	Flash Point	1042.8ºC
Symbol	GHS08	Signal Word	Danger

Names

Name	histrelin
Synonym	More Synonyms

Histrelin BiologicalActivity

Description	Histrelin, a GnRH analogue, is a GnRH Receptor agonist. Histrelin increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin can be used in the research of prostate cancer, endometriosis[1][2][5].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>GNRH ReceptorResearch Areas >>Cancer
Target	GnRH Receptor[1]
In Vitro	Histrelin (10-100 nM) stimulates the release of vasopressin (VP) from from isolated rat hypothalamo-neurohypophysial explants[4]. Histrelin (100 nM) stimulates oxytocin (OT) release from the rat hypothalamo-neurohypophysial system[5].
In Vivo	Histrelin (0.1 mg/kg, subcutaneous injection) rescues the circulating LH concentrations in Csfmop/Csfmop mice[2]. Histrelin (10,30, or 100 μg /day, subcutaneous injection) reduces the number of endometrial glands and atrophied the stroma in rabbits[3]. Animal Model: Csfmop/Csfmop mice [2] Dosage: 0.001, 0.05, and 0.1 mg/kg Administration: Subcutaneous injection Result: Increased serum FSH concentrations by 4-fold. Animal Model: Rabbits[3] Dosage: 10, 30, or 100 μg /day Administration: Subcutaneous injection for 4 weeks Result: Caused a regression of the endometrial glands and a thinning of the stroma.
References	[1]. Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30. [2]. P E Cohen, et al. Colony-stimulating factor-1 plays a major role in the development of reproductive function in male mice. Mol Endocrinol. 1997 Oct;11(11):1636-50. [3]. D W Hahn, et al. Development of an animal model for quantitatively evaluating effects of drugs on endometriosis. Fertil Steril. 1985 Sep;44(3):410-5. [4]. E Boczek-Leszczyk, et al. Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J Physiol Pharmacol. 2010 Aug;61(4):459-66. [5]. Marlena Juszczak, et al. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res Bull. 2010 Jan 15;81(1):185-90.

Chemical & Physical Properties

Density	1.5±0.1 g/cm3
Boiling Point	1800.6ºC at 760 mmHg
Molecular Formula	C₆₆H₈₆N₁₈O₁₂
Molecular Weight	1323.502
Flash Point	1042.8ºC
Exact Mass	1322.667236
PSA	446.86000
LogP	0.09
Index of Refraction	1.701
InChIKey	HHXHVIJIIXKSOE-QILQGKCVSA-N
SMILES	CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(Cc1cn(Cc2ccccc2)cn1)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1c[nH]c2ccccc12)NC(=O)C(Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OK6370800

CHEMICAL NAME :: Luteinizing hormone releasing factor (pig), 6-(1-(phenylmethyl)-D-histidine)-9-(N-ethyl-L- prolinamide)-10-deglycinamide-

CAS REGISTRY NUMBER :: 76712-82-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C66-H86-N18-O12

MOLECULAR WEIGHT :: 1323.70

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 46 ug/kg

SEX/DURATION :: male 2 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male

REFERENCE :: JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 4667 ug/kg

SEX/DURATION :: male 8 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

REFERENCE :: JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2333 ug/kg

SEX/DURATION :: male 4 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

REFERENCE :: JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986

Safety Information

Symbol	GHS08
Signal Word	Danger
Hazard Statements	H360
Precautionary Statements	P201-P308 + P313
Personal Protective Equipment	Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
Hazard Codes	T: Toxic;
Risk Phrases	R60
Safety Phrases	53-22-36/37/39-45
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	OK6370800
HS Code	2937190090

Customs

HS Code	2937190090

Articles42

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...

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...

Treatment and outcomes of precocious puberty: an update.

J. Clin. Endocrinol. Metab. 98(6) , 2198-207, (2013)

Precocious puberty is a common problem affecting up to 29 per 100,000 girls per year. The earliest identified neuroendocrine change in early puberty thus far is increased kisspeptin secretion from the...

Synonyms

histreline

6-(1-(Phenylmethyl)-D-histidine)-9-(N-ethyl-L-prolinamide)-10-deglycinamideluteinizing hormone-releasing fFactor

histrelinum

HISTRELIN

5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide

L-Prolinamide, 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-(phenylmethyl)-D-histidyl-L-leucyl-L-arginyl-N-ethyl-

MFCD00133494

histrelina

(Des-Gly10,His(Bzl)6,Pro-NHEt9)-LHRH

Recommended......