| Description |
Leuprolide acetate (Leuprorelin) is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors. IC50 Value: Target: GnRH receptor 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 |
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| Clinical Trial |
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| References |
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| Preparing Stock Solutions |
Please refer to the solubility information to select the appropriate solvent.
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| References |
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| Molecular Weight |
1269.45 |
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| Formula |
C₆₁H₈₈N₁₆O₁₄ |
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| CAS No. |
74381-53-6 |
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| Storage |
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| Shipping | Room temperature in continental US; may vary elsewhere |
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| Solvent & Solubility |
DMSO: ≥ 43.4 mg/mL
* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> |
Purity: 99.88%
COA (98 KB) HNMR (206 KB) RP-HPLC (165 KB)
Handling Instructions (1252 KB)-
[1]. Mizutani T, Sugihara A, Nakamuro K, Suppression of cell proliferation and induction of apoptosis in uterine leiomyoma by gonadotropin-releasing hormone agonist (leuprolide acetate). J Clin Endocrinol Metab. 1998 Apr;83(4):1253-5.
[2]. Silva AL, Abreu LG, Rosa-e-Silva AC, Leuprolide acetate reduces both in vivo and in vitro ovarian steroidogenesis in infertile women undergoing assisted reproduction. Steroids. 2008 Dec 22;73(14):1475-84.
[3]. Guzmán-Soto I, Salinas E, Hernández-Jasso I, Leuprolide acetate, a GnRH agonist, improves experimental autoimmune encephalomyelitis: a possible therapy for multiple sclerosis. Neurochem Res. 2012 Oct;37(10):2190-7.
[4]. Gaikwad U, Parle M, Kumar A, Effect of ritanserin and leuprolide alone and combined on marble-burying behavior of mice. Acta Pol Pharm. 2010 Sep-Oct;67(5):523-7.
