SyROSingopine 是MCT1和MCT4双重抑制剂,对 MCT4 的效力高 60 倍,可防止乳酸和 H+ 流出。它是可口服抗高血压药物,联合二甲双胍具有研究癌症疾病的潜力。
产品描述
Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor.
体外活性
The anticancer activity of the widely used diabetic drug metformin is strongly potentiated by Syrosingopine. Synthetic lethality elicited by combining the two drugs is synergistic and specific to transformed cells. This effect is unrelated to Syrosingopine??s known role as an inhibitor of the vesicular monoamine transporters. Syrosingopine binds to the glycolytic enzyme α±-enolase in vitro, and the expression of the γ-enolase isoform correlates with nonresponsiveness to the drug combination. Syrosingopine sensitized cancer cells to metformin and its more potent derivative phenformin far below the individual toxic threshold of each compound[1]
Cas No.
84-36-6
分子式
C35H42N2O11
分子量
666.71
储存和溶解度
DMSO:62.5 mg/mL (93.74 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years