Cycloleucine
(Synonyms: 环亮氨酸) 目录号 : GC61751Cycloleucine是一种S-腺苷甲硫氨酸介导的甲基化的特异性抑制剂。Cycloleucine是NMDA受体甘氨酸变构位点的拮抗剂,Ki值为600μM。Cycloleucine在体外也是ATP:L-蛋氨酸-S-腺苷基转移酶的竞争性抑制剂。Cycloleucine具有抗焦虑和抑制细胞作用。
Cas No.:52-52-8
Sample solution is provided at 25 µL, 10mM.
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects[1][2][3][4].
Cycloleucine (4-40 mM; 3 h) blocks internal methylation of viral RNA in B77 transformed chick embryo fibroblasts[5].Cycloleucine (40 mM; 24 h) blocks the formation of both m6A and the penultimate Gm in B77 38S RNA subunits by greater than 90%[5].Cytostatic (10 µg/mL) inhibits the viability human KB and mouse L1210s leukemia cell lines[5].
Cycloleucine (0.5-4 µg; intracerebroventrical injection) increases time spent in open arms, open arm entries, and extreme arrivals in rats[3]. Animal Model: Male rats bilaterally cannulated into the nucleus accumbens septi (NAS)[3]
[1]. Hood WF, et, al. 1-Aminocyclobutane-1-carboxylate (ACBC): a specific antagonist of the N-methyl-D-aspartate receptor coupled glycine receptor. Eur J Pharmacol. 1989 Feb 28;161(2-3):281-2. [2]. Caboche M, et, al. RNA methylation and control of eukaryotic RNA biosynthesis. Effects of cycloleucine, a specific inhibitor of methylation, on ribosomal RNA maturation. Eur J Biochem. 1977 Mar 15;74(1):19-29. [3]. Gargiulo API, et, al. Effects of Cycloleucine in the Nucleus Accumbens Septi on the Elevated plus Maze Test in Rats. Neuropsychobiology. 2020;79(3):191-197. [4]. Du? D, et, al. Cytostatic activity in vitro of cycloleucine, aspartic acid and glutamic acid phosphonic analogues. Arch Immunol Ther Exp (Warsz). 1980;28(3):433-8. [5]. Dimock K, et, al. Cycloleucine blocks 5'-terminal and internal methylations of avian sarcoma virus genome RNA. Biochemistry. 1978 Aug 22;17(17):3627-32.
Cas No. | 52-52-8 | SDF | |
别名 | 环亮氨酸 | ||
Canonical SMILES | O=C(O)C1(CCCC1)N | ||
分子式 | C6H11NO2 | 分子量 | 129.16 |
溶解度 | Water: 50 mg/mL (387.12 mM); DMSO: < 1 mg/mL (ultrasonic) (insoluble or slightly soluble) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 7.7423 mL | 38.7117 mL | 77.4234 mL |
5 mM | 1.5485 mL | 7.7423 mL | 15.4847 mL |
10 mM | 0.7742 mL | 3.8712 mL | 7.7423 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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