Description Background
ChemicalBook > CAS DataBase List > Histrelin

Histrelin

Description Background
Product Name
Histrelin
CAS No.
76712-82-8
Chemical Name
Histrelin
Synonyms
histrelin acetate;PYR-HIS-TRP-SER-TYR-D-HIS(BZL)-LEU-ARG-PRO-NHET;1-9-LUTEINIZING HORMONE-RELEASING FACTOR (SWINE), 6-[1-(PHENYLMETHYL)-D-HISTIDINE]-9-(N-ETHYL-L-PROLINAMIDE)-;N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1-[2-(ethylcarbamoyl)-1-pyrrolidinyl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-[1-(phenylmethyl)-4-imidazoly;orf17070;Supprelin;RWJ-17070;HISTRELIN;Amyridine;Histreline Acetate
CBNumber
CB8480046
Molecular Formula
C66H86N18O12
Formula Weight
1323.53
MOL File
76712-82-8.mol
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Histrelin Property

alpha 
D20 -33.9° (c = 1 in acetic acid)
Density 
1.46±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Aqueous Acid (Slightly), DMSO (Slightly), Methanol (Slightly)
form 
powder
pka
9.82±0.15(Predicted)
Sequence
{Pyr}-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt
Stability:
Hygroscopic
InChIKey
HHXHVIJIIXKSOE-HMGGNIPDNA-N
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Safety

Hazard Codes 
T
Risk Statements 
60
Safety Statements 
53-22-36/37/39-45
WGK Germany 
3
RTECS 
OK6370800
HS Code 
3504009000
Hazardous Substances Data
76712-82-8(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H360May damage fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P308+P313IF exposed or concerned: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
L2761
Product name
[des-Gly10, D-His(Bzl)6]-LH-RH ethylamide
Purity
≥97% (HPLC), powder
Packaging
0.5mg
Price
$162
Updated
2025/07/31
Sigma-Aldrich
Product number
L2761
Product name
[des-Gly10, D-His(Bzl)6]-LH-RH ethylamide
Purity
≥97% (HPLC), powder
Packaging
1mg
Price
$263.65
Updated
2025/07/31
American Custom Chemicals Corporation
Product number
API0002921
Product name
HISTRELIN
Purity
95.00%
Packaging
1MG
Price
$645.9
Updated
2021/12/16
Biorbyt Ltd
Product number
orb372383
Product name
Histrelin Acetate
Purity
> 95%
Packaging
1mg
Price
$691.9
Updated
2021/12/16
Apolloscientific
Product number
BITH3026
Product name
Histrelin
Packaging
25mg
Price
$719
Updated
2021/12/16
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Histrelin Chemical Properties,Usage,Production

Description

Histrelin, a synthetic gonadotrophin-releasing hormone (GnRH) agonist, was introduced as a first-line therapy for the treatment of central precocious puberty. When administered over a prolonged period, it suppresses the release of gonadotrophin, inhibits ovarian and testicular steroidogenesis, and prevents sexual maturation. Superior to the traditional therapy with progestational agents, histrelin appears to have decelerating effects on skeletal maturation allowing more statural growth and significantly increased final adult height. Histrelin has also been used to treat other disorders including endometriosis, polycystic ovarian disease, uterine leiomyomas, severe premenstrual syndrome and to prevent acute intermittent porphyria.

Chemical Properties

[α]D20-33.9°(C=1, acetic acid).

Originator

Johnson & Johnson (U.S.A.)

Uses

LHRH agonist.

Uses

[des-Gly10, D-His(Bzl)6]-LH-RH ethylamide has been used:

  • for inducing Batrachoseps gravid females to oviposit
  • for comparing the effect of LHRH (luteinizing hormone-releasing hormone) agonists and dopamine antagonists in Lithobates pipiens
  • for inducing oviposition in females of Taricha granulosa and Ensatina eschscoltzii
  • to induce spawning in Spea hammondii adults

Definition

ChEBI: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, 1-benzyl-D-histidyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotro in-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the diacetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.

brand name

Supprelin (Roberts Pharmaceutical).

Biochem/physiol Actions

Glp-His-Trp-Ser-Tyr-His(Bzl)-Leu-Arg-Pro-NHEt ([des-Gly10, D-His(Bzl)6]-LH-RH) is a GnRH (gonadotropin-releasing hormone) agonist, histerelin. GnRH (Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), which is also referred as LHRH (luteinizing hormone-releasing hormone) or gonadorelin, is crucial for mammalian reproduction and is released from hypothalamic neurons. It is responsible for the secretion of gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), from the pituitary glands. Mutations in GnRH are associated with normosmic congenital hypogonadotropic hypogonadism. Histerelin is used for the treatment of central precocious puberty in children. It inhibits actions of sex steroids on the male and female reproductive organs.

Description

Histrelin has a molecular formula of C66H86N18O12, a.a. sequence of Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt and having a Mw of 1323.32 Dalton.

Background

Histrelin is a hormone similar to one normally released from the hypothalamus gland in the brain. Histrelin works by decreasing the amount of estrogen and testosterone in the blood. Suppressing estrogen can cause thinning of the bones or slowing of their growth. Histrelin acetate is a potent LHRH agonist which stimulates LH and FSH release and inhibits the actions of sex steroids on the male and female reproductive tracts. After a transient increase, continuous administration results in down regulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis. Histrelin potency in vivo and in vitro is similar to that of the D-Trp6-containing analog. Especially because of its high water solubility and greater lipophilic character, it appears promising for clinical application.

Histrelin Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Histrelin manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Histrelin Acetate 76712-82-8
Price
US $0.00/g
Min. Order
1g
Purity
98%min
Supply Ability
1000g
Release date
2023-01-12
Zhuozhou Wenxi import and Export Co., Ltd
Product
Histrelin 76712-82-8
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-06-27
Career Henan Chemical Co
Product
Histrelin 76712-82-8
Price
US $7.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000KG
Release date
2019-08-31

76712-82-8, HistrelinRelated Search:


  • N-[1-[[1-[[1-[[1-[[1-[[1-[[5-(diaminomethylideneamino)-1-[2-(ethylcarbamoyl)-1-pyrrolidinyl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-[1-(phenylmethyl)-4-imidazoly
  • 1-9-LUTEINIZING HORMONE-RELEASING FACTOR (SWINE), 6-[1-(PHENYLMETHYL)-D-HISTIDINE]-9-(N-ETHYL-L-PROLINAMIDE)-
  • Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt acetate salt
  • 5-oxo-L-pmlyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-N^<T>^-benzyl-D-histidyl-L-leucyl-L-arginyl-N-ethyl-L-pmlinamide
  • RWJ-17070
  • Supprelin
  • 5-Oxo-L-Pro-L-His-L-Trp-L-Ser-L-Tyr-1-benzyl-D-His-L-Leu-L-Arg-L-Pro-N-ethyl-NH2
  • Histreline Acetate
  • ((imbl)-d-his(sub6),pro(sub9)-net)lhrh
  • (n-ethyl-l-prolinamide)-10-deglycinamide-
  • 6-(1-(phenylmethyl)-d-histidine)-9-luteinizinghormonereleasingfactor(pig
  • orf17070
  • PYR-HIS-TRP-SER-TYR-HIS(BZL)-LEU-ARG-PRO-NHET
  • PYR-HIS-TRP-SER-TYR-D-HIS(BZL)-LEU-ARG-PRO-NHET
  • PGLU-HIS-TRP-SER-TYR-D-HIS[BZL]-LEU-ARG-PRO-NHET
  • (HIS(BZL)6)-HISTRELIN
  • HISTRELIN
  • histrelin acetate
  • (DES-GLY10,HIS(BZL)6,PRO-NHET9)-GONADOTROPIN-RELEASING HORMONE
  • (DES-GLY10,HIS(BZL)6,PRO-NHET9)-LHRH
  • (DES-GLY10,HIS(BZL)6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING FACTOR
  • (DES-GLY10,HIS(BZL)6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING HORMONE
  • DES-GLY10,[D-HIS(BZL)6]-LH-RH ETHYLAMIDE
  • (DES-GLY10,D-HIS(BZL)6,PRO-NHET9)-GONADOTROPIN-RELEASING HORMONE
  • (DES-GLY10,D-HIS(BZL)6,PRO-NHET9)-LHRH
  • [DES-GLY10, D-HIS(BZL)6, PRO-NHET9]-LH-RH (HUMAN)
  • (DES-GLY10,D-HIS(BZL)6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING FACTOR
  • (DES-GLY10,D-HIS(BZL)6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING HORMONE
  • [DES-GLY10, D-HIS(BZL)6, PRO-NHET9]-LUTEINIZING HORMONE-RELEASING HORMONE (HUMAN)
  • Histrelin USP/EP/BP
  • Histrelin Acetate(net)
  • Amyridine
  • [des-Gly<sup>10</sup>, <sc>D</sc>-His(Bzl)<sup>6</sup>]-LH-RH ethylamide
  • 76712-82-8
  • C66H86N18O12
  • Biochemicals and Reagents
  • Amino Acids and Peptides
  • BioChemical
  • Peptides
  • Releasing Factors
  • LH-RH
  • hormones
  • Peptide