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大鼠和小鼠中的强效 LHRH 类似物。Alarelin 可逆地延迟大鼠的性成熟。作为单一药物或与多巴胺受体拮抗剂联合应用,如多潘立酮,用于刺激和同步排卵和鱼类养殖产卵。CAS号(净):79561-22-1。
编号:167572
CAS号:148029-26-9/79561-22-1
单字母:Pyr-HWSYaLRP-NHEt
| 编号: | 167572 |
| 中文名称: | 醋酸阿拉瑞林、Alarelin Acetate |
| 英文名: | Alarelin Acetate |
| CAS号: | 148029-26-9,freebase 79561-22-1,醋酸盐 |
| 单字母: | Pyr-HWSYaLRP-NHEt |
| 三字母: | Pyr 焦谷氨酸(Glp、pGlu、Pyr)是一种在蛋白质N端位置发现的蛋白质生成氨基酸。它是由N端谷氨酸残基环化形成内酰胺而产生的。 -HisL-组氨酸:histidine。系统命名为(2S)-氨基-3-(4-咪唑基)丙酸。其侧链带有弱碱性的咪唑基,为编码氨基酸。是幼小哺乳动物的必需氨基酸。符号:H,His。 -TrpL-色氨酸:tryptophan[e]。系统命名为(2S)-氨基-3-(3-吲哚基)丙酸。是编码氨基酸,哺乳动物的必需氨基酸。符号:W,Trp。某些抗菌素中含有 D-色氨酸。 -SerL-丝氨酸:serine。系统命名为(2S)-氨基-3-羟基丙酸。是编码氨基酸。因可从蚕丝中获得而得名。符号:S,Ser。在丝原蛋白及某些抗菌素中含有 D-丝氨酸。 -TyrL-酪氨酸:tyrosine。系统命名为(2S)-氨基-3-(4-羟基苯基)丙酸。是编码氨基酸。符号:Y,Tyr。 -DAlaD型丙氨酸 -LeuL-亮氨酸:leucine。系统命名为(2S)-氨基-4-甲基戊酸。是编码氨基酸。是哺乳动物的必需氨基酸。符号:L,Leu。 -ArgL-精氨酸:arginine。系统命名为(2S)-氨基-5-胍基戊酸。在生理条件下带正电荷,为编码氨基酸。是幼小哺乳动物的必需氨基酸。符号:R,Arg。 -ProL-脯氨酸:proline。系统命名为吡咯烷-(2S)-羧酸。为亚氨基酸。是编码氨基酸。在肽链中有特殊作用,如易形成顺式的肽键等。符号:P,Pro。 -NHEtC端乙胺基化修饰 |
| 氨基酸个数: | 8 |
| 分子式: | C56H78N16O12 |
| 平均分子量: | 1167.32 |
| 精确分子量: | 1166.6 |
| 等电点(PI): | - |
| pH=7.0时的净电荷数: | 2.24 |
| 酸性基团个数: | 1.1 |
| 碱性基团个数: | 疏水 |
| 平均亲水性: | -0.9 |
| 疏水性值: | -0.79 |
| 外观与性状: | 白色粉末状固体 |
| 消光系数: | 6990 |
| 来源: | 人工化学合成,仅限科学研究使用,不得用于人体。 |
| 纯度: | 95%、98% |
| 盐体系: | 可选TFA、HAc、HCl |
| 储存条件: | 负80℃至负20℃ |
| 标签: | D型氨基酸肽 瑞林类 |
Potent LHRH analog in rats and mice. Alarelin reversibly delays sexual maturation in rats.Applied as single drug or in combination with a dopamin receptor antagonist as domperidone for the stimulation and synchronization of ovulation and spawning in fish farming. CAS Number (net): 79561-22-1.
阿拉瑞林,D - 丙氨酸 6, 去甘氨酸 10 促黄体生成素释放激素乙基酰胺引入立体化学和缺失修饰,改变主链几何。该肽保留结构和结合研究必需残基。其酰胺化形式增强构象稳定性。研究人员将其用于类似物设计、构效评估和基序功能研究。
Alarelin, DAla6,Des-Gly10 LH-RH, Ethyl Amide introduces stereochemical and deletion modifications that reshape backbone geometry. The peptide retains essential residues for structural and binding investigations. Its amidated form enhances conformational stability. Researchers employ it in analog design, structure-activity evaluation, and motif-function studies.
很多蛋白在细胞中非常容易被降解,或被标记,进而被选择性地破坏。但含有部分D型氨基酸的多肽则显示了很强的抵抗蛋白酶降解能力。
| DOI | 名称 | |
|---|---|---|
| 10.1016/s0014-827x(02)01295-8 | Sustained release and biological availability of dalarelin from the biodegradable coacervate microcapsules | 下载 |
| 10.1210/en.2004-0558 | Novel expression of gonadotropin subunit genes in oocytes of the gilthead seabream (Sparus aurata) | 下载 |
| 10.1002/jms.1416 | In vivo evaluation and in vitro metabolism of leuprolide in mice--mass spectrometry-based biomarker measurement for efficacy and toxicity | 下载 |
| 10.1016/j.cbpa.2010.11.016 | Effects of in vivo treatment with the dopamine antagonist pimozide and gonadotropin-releasing hormone agonist (GnRHa) on the reproductive axis of Senegalese sole (Solea senegalensis) | 下载 |
| 10.1016/j.ygcen.2011.10.013 | Dopamine control of LH release in the tench (Tinca tinca) | 下载 |
| 10.1016/j.ygcen.2013.06.005 | Chronic kisspeptin administration stimulated gonadal development in pre-pubertal male yellowtail kingfish (Seriola lalandi; Perciformes) during the breeding and non-breeding season | 下载 |
| 10.1021/bc500081g | GnRH-Gemcitabine conjugates for the treatment of androgen-independent prostate cancer: pharmacokinetic enhancements combined with targeted drug delivery | 下载 |
| 10.1016/s0016-6480(89)80045-0 | Control of gonadotropin release in the Atlantic croaker (Micropogonias undulatus): evidence for lack of dopaminergic inhibition | 下载 |
| 10.1095/biolreprod32.2.226 | D-Ala6-des-Gly10-gonadotropin-releasing hormone ethylamide: absence of binding sites and lack of a direct effect in rabbit corpora lutea | 下载 |
| 10.1210/endo-100-4-918 | Insensitivity of bonnet monkeys to (D-Ala6, Des-Gly10) LHRH ethylamide, a potent new luteinizing hormone releasing hormone analogue in rats and mice | 下载 |





