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。
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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。 |
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]. |
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 |
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 |