Leuprolide Acetate

- Overview
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    Background
    
    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
- Properties
  - Categories
    
    Pituitary GnRH receptors agonist
    
    Alternative Name
    
    Leuprorelin acetate;Lupron; Leuprorelin acetate;Lupron
    
    CAS Number
    
    74381-53-6
    
    Molecular Formula
    
    C61H88N16O14
    
    Molecular Weight
    
    1269.45
    
    Appearance
    
    A solid
    
    Purity
    
    99.85%
    
    Solubility
    
    ≥126.9 mg/mL in DMSO; ≥102 mg/mL in H2O with gentle warming; ≥31.4 mg/mL in EtOH with gentle warming
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N6.CC(=O)O
    
    * For Research Use Only