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Leuprorelin Acetate,53714-56-0

Leuprorelin Acetate,53714-56-0
  • CAS#:53714-56-0
  • Product Name:Leuprorelin Acetate
  • Size:1g or more
  • Supply Ability:500g/two weeks
  • FOB Price:Email
  • Payment Terms:T/T
  • Lead time:Within 12 hours after receiving payment
  • Packing:Discreet ways of packing for Customs pass guaranteed
  • Delivery:by express (FedEx,UPS,DHL,EMS), by air
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Leuprorelin Acetate-Physiochemical properties

      Alternate Names:Leuprorelin Acetate,(Des-Gly10,D-Leu6,Pro-NHEt9)-LHRH ,LH-RH LEUPROLIDE;LEUPROLIDE;LEUPROLIDE (HUMAN);LEUPRORELIN;[DES-GLY10, D-LEU6, PRO-NHET9]-LUTEINIZING HORMONE-RELEASING HORMONE HUMAN;(DES-GLY10,D-LEU6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING HORMONE;(DES-GLY10,D-LEU6,PRO-NHET9)-LUTEINIZING HORMONE-RELEASING FACTOR;[DES-GLY10, D-LEU6, PRO-NHET9]-LH-RH (HUMAN)

      Sequence(Single-Letter Code): Pyr- HWSY(d)LLRP -NHEt

      Sequence(Three-Letter Code): pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt

      Molecular Formula: C61H88N16O14

      Molecular weight: 1269.45 g/mol

      Storage:store in cool, dry, ventilated place

      PSA:     466.34000

      LogP:     3.44730

Leuprorelin Acetate Description

Leuprolide Acetate is a potent LHRH (GnRH) agonist. After a transient increase, continuous administration of leuprolide results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis. Studies with female Alzheimer patients indicate that application of leuprolide acetate in combination with an acetylcholinesterase inhibitor stabilizes the cognitive functions in mild-to-moderate cases.

Description: IC50 Value: N/A Leuprorelin (INN) or leuprolide acetate (USAN) is a GnRH analog. leuprolide acetate acts as an agonist at pituitary GnRH receptors. By interrupting the normal pulsatile stimulation of, and thus desensitizing, the GnRH receptors, it indirectly downregulates the secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to hypogonadism and thus a dramatic reduction in estradiol andtestosterone levels in both sexes. in vitro: The number of DNA 3'-end-labeled cells/cm2 in leiomyomas of control patients and in leiomyomas at the 2nd, 8th, 12th, and 16th weeks of Leuprolide Acetate treatment were at low levels [1]. Testosterone, estradiol and progesterone were also reduced by LA, even though this reduction occurred for progesterone only at the highest LA dosage (10(-6)M; 606.0+/-114.3 ng/ml versus 1524.0+/-246.5 ng/ml; p=0.02) [2]. in vivo: Leuprolide acetate treatment decreases the severity of clinical signs of locomotion, induces a significantly greater body weight gain, increases the MBP and NFs expression, axonal area and cell infiltration in EAE animals [3]. Leuprolide (200 and 300 microg kg(-1) s.c.) per se showed anti-compulsive effect, causing statistically significant inhibition of marble-burying behavior of mice [4]. Clinical trial: Neoadjuvant Abiraterone Acetate Plus Leuprolide Acetate in Men With Localized High Risk Prostate Cancer . Phase 2


Leuprorelin acetate is a GnRH sequence that acts as an antagonist for pituitary GnRH receptors in animals. Using this to interrupt the regular pulsatile of this chemical desensitizes GnRH receptors, to down-regulate the gonadotropins of LH and FSH. This will lead to hypogonadism which will dramatically reduce testosterone and estradiol.

Research of leuprorelin acetate typically revolves around its potential use in managing hormone responsive cancers such as breast or prostate cancer as well as conditions that are dependent on estrogen such as endometriosis. Some research indicates that leuprorelin may have use in managing precocious puberty or controlling the stimulation of the ovaries. Some research has looked into the potential for using leuprorelin acetate to reduce sexual urges as displayed by pedophiles or sex offenders.

Non-sexual research into leuprorelin includes the potential management of Alzheimer’s disease. Research involving ferrets has implied that chronic adrenal disease could also be managed by administering leuprorelin acetate. Some research focuses on the potential to use leuprorelin acetate as a means to manage autism, but this was based on the assumption that testosterone or mercury played a hand in developing this disease, which has been revealed to be untrue.

Leuprorelin Acetate Application

Advanced hormone-dependent prostate cancer
Advanced hormone-dependent breast cancer
Endometriosis
Uterine myoma
Central precocious puberty

Leuprorelin Acetate References

 
1, Merck Index, 15th ed., No. 5509, , (2013)
2,D.Levine et al., J. Reprod. Med., 52, 581 (2007)
3,E.Castellón et al., Cancer Invest., 24, 261 (2006)
4,A.Imai et al., Int. J. Oncol., 20, 987 (2002)
5,J.D.Meyer et al., J. Pept. Res., 60, 159 (2002)
6,T.Mizutani et al., Int. J. Fertil. Menopaus. Stud., 40, 106 (1995)
7,P.Chrisp and E.M.Sorkin, Drugs & Aging, 1, 487 (1991)
8,A.S.Dutta, Drugs Future, 13, 43 (1988)
9,D.H.Coy and A.V.Schally, Ann. Clin. Res., 10, 139 (1978)

 

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