地加瑞克醋酸盐
醋酸地加瑞克(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-ly)
CAS: 214766-78-6
化学式: C82H103ClN18O16
| 中文名 | 醋酸地加瑞克 |
| 英文名 | 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-ly |
| 别名 | 地加瑞克 醋酸地加瑞克 地加瑞克-D7 地加瑞克醋酸盐 DEGARELIX游离 |
| 英文别名 | FirMagon Firmagon Degarelix DEGARELIX Degarelix acetate Degarelix acetate salt Degarelix, Degarelix acetate Degarelix acetate(FE-200486,Degarelix) N-Acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-4-[2,6-dioxohexahydropyrimidin-4(S)-ylcarboxamido]-L-phenylalanyl-4-ureido-D-phenylalanyl-L-leucyl-N6-isopropyl-L-lysyl-L-prolyl-D-alaninamide acetate 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-ly D-Alaninamide, N-acetyl-3-(naphtalen-2-yl)-D-alanyl-4-chloro-D-phenylalanyl-3-(pyridin-3-yl)-D-alanyl-L-seryl-4-((((4S)-2,6-dioxohexahydropyrimidin-4-yl)carbonyl)amino)-L-phenylalanyl-4-(carbamoylamino)-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl- |
| CAS | 214766-78-6 |
| EINECS | 807-277-4 |
| 化学式 | C82H103ClN18O16 |
| 分子量 | 1632.26 |
| 密度 | 1.325±0.06 g/cm3(Predicted) |
| 酸度系数 | 10.38±0.40(Predicted) |
| 存储条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| 体外研究 | Degarelix acts directly on the pituitary receptors for luteinizing hormone-releasing hormone (LHRH), blocking the action of endogenous LHRH. The use of degarelix eliminates the initial undesirable surge in gonadotropin and testosterone levels, which is produced by agonists of LHRH. Degarelix treatment reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells), with the exception of the PC-3 cells. The GnRH antagonist degarelix exerts a direct effect on prostate cell growth through apoptosis. |
| 体内研究 | At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increases with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively. 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%). |
地加瑞克醋酸盐 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.613 ml | 3.063 ml | 6.126 ml |
| 5 mM | 0.123 ml | 0.613 ml | 1.225 ml |
| 10 mM | 0.061 ml | 0.306 ml | 0.613 ml |
| 5 mM | 0.012 ml | 0.061 ml | 0.123 ml |
最后更新：2024-01-02 23:10:35
地加瑞克醋酸盐 - 简介
性质：
醋酸地加瑞克是一种无色、有弱酸性的液体，在常温下具有刺激性气味。它具有较高的挥发性和易燃性，与水混溶。
用途：
制法：
醋酸地加瑞克的常用制备方法是通过乙酸和异丁烯醇的酯化反应得到。反应中使用硫酸作为催化剂，并进行适当的温度和反应时间控制。
安全信息：
醋酸地加瑞克具有挥发性和易燃性，应远离明火及其他热源，并储存在阴凉干燥的地方。
使用时需佩戴适当的防护措施，如戴手套、护目镜和防护服等。
在密闭的环境中使用或处理时，需确保良好的通风条件。
避免与皮肤、眼睛和呼吸道接触，如不慎接触，请立即用大量清水冲洗，并及时就医。
在使用醋酸地加瑞克时，请务必遵循正确的操作方法和安全措施，以确保人身安全和实验室环境的安全。
最后更新：2024-04-09 02:00:07
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