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环亮氨酸 /Cycloleucine {[allProObj[0].p_purity_real_show]}

货号:A224871 同义名: 1-氨基环戊烷甲酸

Cycloleucine 是一种特异性的 S-腺苷甲硫氨酸介导的甲基化抑制剂,也是 NMDA 受体甘氨酸变构位点的拮抗剂,Ki 值为 600 μM。此外,它在体外是 ATP:L-蛋氨酸-S-腺苷基转移酶的竞争性抑制剂,具备抗焦虑和抑制细胞的作用。

Cycloleucine 化学结构 CAS号:52-52-8
Cycloleucine 化学结构
CAS号:52-52-8
Cycloleucine 3D分子结构
CAS号:52-52-8
Cycloleucine 化学结构 CAS号:52-52-8
Cycloleucine 3D分子结构 CAS号:52-52-8
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Cycloleucine 纯度/质量文件 产品仅供科研

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产品名称 AMPA receptor GluR mGluR5 NMDA receptor 其他靶点 纯度
Evans Blue 85% (Dye content)
IEM-1754 +

GluR1, IC50: 6 μM

GluR3, IC50: 6 μM

99%
Latrepirdine 2HCl 98%
(-)-Huperzine A +++

AChE (G4 form), Ki: 7 nM

98%
CTEP ++++

mGlu5, IC50: 2.2 nM

98%+
MPEP ++

mGluR5, IC50: 36 nM

99%+
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Cycloleucine 生物活性

描述 Cycloleucine acts as a specific blocker of S-adenosyl-methionine dependent methylation processes and antagonizes the NMDA receptor-associated glycine receptor, evidenced by a Ki value of 600 μM. It also competitively inhibits ATP: L-methionine-S-adenosyl transferase in vitro, displaying anxiolytic and cytostatic effects[1].[2].[3].[4].
体内研究

Administered intracerebroventricularly at doses between 0.5 and 4 μg, cycloleucine enhances exploratory behavior in rats, as shown by increased time spent in open arms, more entries into open arms, and increased extreme arrivals during tests[3].

Additionally, cycloleucine leads to a reduction in the weights of the thymus and spleen in both infected and control mice exposed to the Semliki Forest virus (SFV) strain A7(74)[6].

体外研究

Treatment with cycloleucine, ranging from 4 to 40 mM for 3 hours, effectively prevents internal methylation of viral RNA in B77 transformed chick embryo fibroblasts[5].

At a concentration of 40 mM for 24 hours, cycloleucine significantly impedes the formation of m6A and the penultimate Gm in the B77 38S RNA subunits by over 90%[5].

Cytostatic, at a dose of 10 μg/mL, diminishes the viability of human KB and mouse L1210s leukemia cell lines[5].

Cycloleucine 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.

Cycloleucine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

7.74mL

1.55mL

0.77mL

38.71mL

7.74mL

3.87mL

77.42mL

15.48mL

7.74mL

Cycloleucine 技术信息

CAS号52-52-8
分子式C6H11NO2
分子量 129.16
别名 1-氨基环戊烷甲酸
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

H2O: 20 mg/mL(154.85 mM),配合低频超声助溶

动物实验配方
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