Terfenadine

SKU: orb1224896

Description

Terfenadine is a histamine H1-receptor antagonist, which blocks HERG and KATP (KIR6) channels. (In Vitro):Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells.Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity.Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms.(In Vivo):Terfenadine (p.o.; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 50679-08-8
• MW: 471.67
• Purity: >98% (HPLC)
• Formula: C₃₂H₄₁NO₂
• SMILES: OC(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2
• Target: 5-HT Receptor
• Solubility: Water: 0.0963 mg/L

Bioactivity

• In Vivo:
  Terfenadine (p.o. ; 40 mg/kg; for 16 days) produces a significant inhibition of tumour growth rate and enhances the anti-cancer effect of EPI in chemo-resistant NSCLC xenograft models. Animal model: 6-week-old male BALB/cA-nu mice. Dosage: 40 mg/kg. Administration: p.o. ; for 16 days. Result: Produced a significant inhibition of tumour growth rate.
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• In Vitro:
  Terfenadine ((±)-Terfenadine) (4-20 μM; 24 hours) induces dose and time-dependent apoptosis on A375 melanoma cells. The IC50 after 24 h of TEF treatment in complete medium was 10.4 μM for A375 cells, 9.9 μM for Hs294T cells and 9.6 for HT144 cells. Terfenadine (2-10 μM; 8 hours) induces dose-dependent cytotoxicity. Terfenadine (10 μM; 8 hours) causes a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages. Terfenadine induces autophagy by ROS-dependent and -independent mechanisms. Apoptosis Analysis Cell line: A375, HT144 and Hs294T cells. Concentration: 4, 8, 12, 16, 20 μM. Incubation time: 24 hours. Result: Induced dose and time-dependent apoptosis. Cell Cytotoxicity Assay Cell line: A375 melanoma cells. Concentration: 2, 4, 6, 8, 10 μM. Incubation time: 8 hours. Result: Induces dose-dependent cytotoxicity. Cell Autophagy Assay Cell line: A375 cells. Concentration: 10 μM. Incubation time: 8 hours. Result: Caused a massive vacuolization of the cytoplasm and autophagic vacuoles of both double and multiple membranes and at various stages.
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Storage & Handling

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

Alternative Names

MDL 9918 | NSC 665802 | (±)-Terfenadine | DL-Terfenadine

Quick Database Links

Gene Symbol

5-HT Receptor