Syrosingopine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

昔洛舍平对脑胺具有选择性消耗作用，与双硫仑或镰刀菌酸（一种多巴胺β-羟化酶抑制剂）联合治疗可增强这种作用。

Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor.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.

Cell Viability Assay Cell Line:HeLa, MCT1-KO, MCT4-KO HAP1, HAP1 MCT1-KO Concentration:10 μM Incubation Time:1, 2, 3, 4 hours Result:Caused intracellular lactate accumulation and acidification.Slowed lactate efflux by inhibiting MCT4 and MCT1. Induced synthetic lethality by inhibiting transport of lactate when combined with metformin.

Animal Model:Spontaneously hypertensive rats (SHR) (2 to 17-month-age).Dosage:5 mg/kg Administration:Subcutaneous injection; once (16 hours before undertaking the study of blood pressure).Result:Showed anti-hypertensive activity by depleting peripheral stores of norepinephrine.

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GPCR/G Protein

Dopamine Receptor

dopamine

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84-36-6

666.71

C35H42N2O11

>98% (HPLC)

DMSO:62.5 mg/mL (93.74 mM; Need ultrasonic)

[H][C@@]12C(NC3=C4C=CC(OC)=C3)=C4CCN1C[C@]5(C[C@@H](OC(C6=CC(OC)=C(OC(OCC)=O)C(OC)=C6)=O)[C@H](OC)[C@@H](C(OC)=O)[C@]5(C2)[H])[H]

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(-20℃)

With Ice Pack

≥ 2 years