Cycloleucine 是 NMDA 受体相关甘氨酸受体的拮抗剂,Ki 为 600 μM。Cycloleucine 也是 S-腺苷甲硫氨酸介导的甲基化的竞争性抑制剂,具有抗焦虑和细胞抑制作用。
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Cycloleucine is an antagonist of NMDA receptor associated glycine receptor with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of S-adenosyl-methionine mediated methylation with anxiolytic and cytostatic effects.
体外活性
Cytostatic (10 μg/mL) inhibits the viability of human KB and mouse L1210s leukemia cell lines. Cycloleucine (4-40 mM; 3 h) blocks internal methylation of viral RNA in B77 transformed chick embryo fibroblasts. Cycloleucine (40 mM; 24 h) blocks the formation of both m6A and the penultimate Gm in B77 38S RNA subunits by greater than 90%[2].
体内活性
Cycloleucine (0.5, 1.0, 2.0, 4 μg/μL; intracerebroventrically) increases time spent in open arms, open arm entries, and extreme arrivals in rats[3]. In Semliki Forest virus strain A7(74) infected and control mice, Cycloleucine reduces thymus and spleen weights[4].
Cas No.
52-52-8
分子式
C6H11NO2
分子量
129.159
储存和溶解度
DMSO:< 1 mg/mL (insoluble or slightly soluble),Need ultrasonic
H2O:45 mg/mL (348.41 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years