Terfenadine-d3

• Description:

  Terfenadine-d3 ((±) -Terfenadine-d3) is the deuterium labeled Terfenadine. 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].

• UNSPSC:

  12352005

• Target:

  Apoptosis; Caspase; Histamine Receptor; Isotope-Labeled Compounds; Na+/Ca2+ Exchanger; Potassium Channel

• Related Pathways:

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

• Applications:

  Metabolism-protein/nucleotide metabolism

• Field of Research:

  Cancer; Inflammation/Immunology; Endocrinology

• Solubility:

  10 mM in DMSO

• Smiles:

  C(O)(C1CCN(CCC(C(O)(C2=CC=C(C(C)(C)C)C=C2)[2H])([2H])[2H])CC1)(C3=CC=CC=C3)C4=CC=CC=C4

• Molecular Formula:

  C32H38D3NO2

• Molecular Weight:

  474.69

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108 (3) :301-307.|[3]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.|[4]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

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• Isoform:

  H1 Receptor

• CAS Number:

  [192584-82-0]