Coptisine chloride

SKU: orb1221983

Description

Coptisine chloride can be absorbed across intestinal epithelial cells, and completely absorbed compounds.

Key Properties

• CAS Number: 6020-18-4
• MW: 355.77
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₄ClNO₄
• SMILES: C1C[N+]2=C(C=C3C=CC4=C(C3=C2)OCO4)C5=CC6=C(C=C51)OCO6.[Cl-]
• Target: PKC
• Solubility: DMSO : 10.75 mg/mL 30.22 mM

Bioactivity

• In Vivo:
  Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD50 value of 880.18 mg/kg. Coptisine (154 mg/kg/day, 90 days) shows no toxicity on SD rats. Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism.
• In Vitro:
  Coptisine chloride is an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC50s of 18.09, 29.50, 21.60, 20.15 and 26.60 μM, respectively. Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 h).

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

PKC