| Identification | Back Directory | [Name]
Unii-I18S89p20r | [CAS]
934246-14-7 | [Synonyms]
Unii-I18S89p20r
Degarelix (acetate H2O)
Degarelix Acetate Hydrate
D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-4-((((4S)-hexahydro-2,6- dioxo-4-pyrimidinyl)carbonyl)amino)-L-phenylalanyl-4-((aminocarbonyl)amino)-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-, acetate, hydrate (1::) | [Molecular Formula]
C84H107ClN18O18 | [MOL File]
934246-14-7.mol | [Molecular Weight]
1692.34 |
| Chemical Properties | Back Directory | [Melting point ]
>230°C (dec.) | [storage temp. ]
Hygroscopic, -20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly) | [form ]
Solid | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
The Acetate salt of Degarelix (D495465) which is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. | [in vivo]
Degarelix (0-10 μg/kg; s.c.; once) decreases plasma LH levels and plasma testosterone levels in a dose-dependent manner in castrated rats[3].
Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rat and dog, most of the degarelix dose is eliminated within 48 h via urine and feces in equal amounts (40–50% in each matrix), whereas in monkey the major route of excretion is fecal (50%) and renal (22%)[4]. | Animal Model: | Male Sprague-Dawley rats, castrated[3] | | Dosage: | 0.3, 1, 3 and 10 μg/kg or 12.5, 50, and 200 μg/kg | | Administration: | Subcutaneous injection, once | | Result: | Produced a dose-dependent and reversible decrease in plasma LH levels with a minimal effective dose of 3 μg/kg.
For the 50 μg/kg and 200 μg/kg doses, t1/2 of absorption values were 4 min and 30 min, Tmax values were 1 h and 5 h, and apparent plasma disappearance t1/2 values were 12 h and 67 h, respectively.
Produced a dose-dependent decrease in plasma testosterone levels with a minimal effective dose of 1 μg/kg.
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