Degarelix acetate hydrate 是一种竞争性的、可逆的促性腺激素释放激素受体 (GnRHR/LHRHR) 拮抗剂。Degarelix acetate hydrate 可用于前列腺癌的研究。
| 生物活性 | Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostatecancerresearch[1]. |
体外研究
(In Vitro) | Degarelix shows only very weak histamine-releasing properties and the lowest capacity for histamine release among the antagonists of LHRH, including Cetrorelix (HY-P0009), Abarelix (HY-13534), and Ganirelix (HY-P1628)[1].
Degarelix (1 nM-10 μM, 0-72 h) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), with the exception of the PC-3 cells[2].
Degarelix (10 μM, 0-72 h) exerts a direct effect on prostate cell growth through apoptosis[2].
Cell Viability Assay[2] | Cell Line: | WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP | | Concentration: | 1 nM-10 μM | | Incubation Time: | WPMY-1 cells at 48 and 72h, WPE1-NA22 cells at 72 hours, BPH-1 cells at 48 and 72h, LNCaP cells at 48 and 72h | | Result: | Reduced cell viability in all prostate cell lines, with the exception of the PC-3 cells. |
Apoptosis Analysis[2] | Cell Line: | WPE1-NA22, BPH-1, LNCaP and VCaP | | Concentration: | 10 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Induced a significant increase on caspase 3/7 activation. |
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体内研究
(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, t1/2of absorption values were 4 min and 30 min, Tmaxvalues were 1 h and 5 h, and apparent plasma disappearance t1/2values 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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| Clinical Trial | |
| Formula | C82H103ClN18O16.xC2H4O2.xH2O |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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