Cycloleucine(Synonyms: 环亮氨酸)

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Cycloleucine (Synonyms: 环亮氨酸) 纯度: ≥98.0%

Cycloleucine 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 600 μM。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。

Cycloleucine(Synonyms: 环亮氨酸)

Cycloleucine Chemical Structure

CAS No. : 52-52-8

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生物活性

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].

IC50 & Target

Ki: 600 μM (NMDA)[1][2]
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Cycloleucine (0.5-4 µg; intracerebroventrical injection) increases time spent in open arms, open arm entries, and extreme arrivals in rats[3]. Cycloleucine reduces thymus and spleen weights in Semliki Forest virus (SFV) strain A7(74) infected and control mice[6].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats bilaterally cannulated into the nucleus accumbens septi (NAS)[3]
Dosage: 1 µL of 0.5, 1.0, 2.0, 4 µg/µL
Administration: Intracerebroventrical injection
Result: Increased time spent in the open arms and extreme arrivals at all doses.
Increased open arm entries at the dose of 4 μg.

分子量

129.16

Formula

C6H11NO2
CAS 号

52-52-8
中文名称

环亮氨酸；1氨基环戊烷甲酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 50 mg/mL (387.12 mM; Need ultrasonic)

DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 7.7423 mL 38.7117 mL 77.4233 mL
5 mM 1.5485 mL 7.7423 mL 15.4847 mL
10 mM 0.7742 mL 3.8712 mL 7.7423 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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]. Duś 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.

    [6]. S Amor, et al. The effect of cycloleucine on SFV A7(74) infection in mice. Br J Exp Pathol. 1987 Apr;68(2):225-35.

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