Terfenadine

• Description:

  Terfenadine ((±) -Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].

• Product Name Alternative:

  (±) -Terfenadine; MDL-991

• UNSPSC:

  12352005

• Hazard Statement:

  H413

• Target:

  Apoptosis; Caspase; Histamine Receptor; Na+/Ca2+ Exchanger; Potassium Channel

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer; Inflammation/Immunology; Endocrinology

• Assay Protocol:

  https://www.medchemexpress.com/Terfenadine.html

• Concentration:

  10mM

• Purity:

  99.98

• Solubility:

  DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL

• Smiles:

  OC(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2

• Molecular Formula:

  C32H41NO2

• Molecular Weight:

  471.67

• Precautions:

  H413

• References & Citations:

  [1]Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108 (3) :301-307.|[2]Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16 (12) :1253-67.|[3]An L, et al. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  Caspase 2; Caspase 4; Caspase 9; H1 Receptor

• CAS Number:

  [50679-08-8]