Levobupivacaine HCl

SKU: orb1225454

Description

Levobupivacaine HCl, the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.(In Vitro):Levobupivacaine (0-4 mM; 24 h) does not affect the viability of GES-1 cells but inhibits the viability of HGC27 and SGC7901 cells.Levobupivacaine (2 mM; 24, 48 or 72 h) enhances Erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induces the levels of Fe2+, iron, and lipid ROS.Levobupivacaine (2 mM; 24 h) enhances the expression of miR-489-3p in HGC27 and SGC7901 cells, increases the levels of Fe2+ and iron.(In Vivo):Levobupivacaine (40 μmol/kg; IP; once daily for 25 days) significantly inhibits SGC7901 cell growth, and enhances the lipid ROS accumulation.Levobupivacaine (5 or 36 mg/kg; IP; single dosage) increases the latency to partial seizures and prevents the occurrence of generalized seizures at low dosage; reduces the latency to N-methyl-d-aspartate (NMDA)-induced seizures and increased seizure severity at high dosage.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 27262-48-2
• MW: 324.89
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₈N₂O·HCl
• SMILES: CCCCN1CCCC[C@H]1C(=O)NC2=C(C=CC=C2C)C.Cl
• Target: Sodium Channel
• Solubility: DMSO:64 mg/mL (196.98 mM); Ethanol:57 mg/mL (175.44 mM); Water:64 mg/mL (196.98 mM)

Bioactivity

• In Vivo:
  Levobupivacaine (40 μmol/kg; IP; once daily for 25 days) significantly inhibits SGC7901 cell growth, and enhances the lipid ROS accumulation. Levobupivacaine (5 or 36 mg/kg; IP; single dosage) increases the latency to partial seizures and prevents the occurrence of generalized seizures at low dosage; reduces the latency to N-methyl-d-aspartate (NMDA)-induced seizures and increased seizure severity at high dosage. Animal model: CD1 mice (30-35 g; induced epileptic seizures by injecting with NMDA). Dosage: 5 or 36 mg/kg. Administration: IP; single dosage. Result: Increased the latency to partial seizures and prevented the occurrence of generalized seizures at 5 mg/kg; reduced the latency to NMDA-induced seizures and increased seizure severity at 36 mg/kg. Animal model: SCID nude mice (6-8 weeks; subcutaneously injected with 5×106 SGC7901 cells). Dosage: 40 μmol/kg. Administration: IP; once daily for 25 days. Result: Significantly inhibited SGC7901 cell growth, and enhanced the lipid ROS accumulation.
• In Vitro:
  Levobupivacaine (0-4 mM; 24 h) does not affect the viability of GES-1 cells but inhibits the viability of HGC27 and SGC7901 cells. Levobupivacaine (2 mM; 24, 48 or 72 h) enhances Erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induces the levels of Fe2+, iron, and lipid ROS. Levobupivacaine (2 mM; 24 h) enhances the expression of miR-489-3p in HGC27 and SGC7901 cells, increases the levels of Fe2+ and iron. Cell Viability Assay Cell line: GES-1, HGC27 and SGC790. Concentration: 0, 0.5, 1, 2 and 4 mM Incubation time: 24 h. Result: Did not affect the viability of normal gastric epithelial GES-1 cell lines but inhibited the viability of HGC27 and SGC7901 cells in a dose-dependent manner. Cell Viability Assay Cell line: HGC27 and SGC7901 (incubated with 5 μM erastin). Concentration: 2 mM. Incubation time: 24, 48 or 72 h. Result: Enhanced erastin-induced inhibitory impact on HGC27 and SGC7901 cell viabilities; induced the levels of Fe2+, iron, and lipid ROS. RT-PCR Cell line: HGC27 and SGC7901 (incubated with 5 μM erastin). Concentration: 2 mM. Incubation time: 24 h. Result: Enhanced the expression of miR-489-3p in HGC27 and SGC7901 cells, increased the levels of Fe2+ and iron.

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

Sodium Channel