Syrosingopine

SKU: orb1219310

Description

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.

Key Properties

• CAS Number: 84-36-6
• MW: 666.71
• Purity: >98% (HPLC)
• Formula: C₃₅H₄₂N₂O₁₁
• SMILES: [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]
• Target: Dopamine Receptor
• Solubility: DMSO:62.5 mg/mL (93.74 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Dopamine Receptor