Terfenadine-d3

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].

192584-82-0

12352005

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

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

Metabolism-protein/nucleotide metabolism

Cancer; Inflammation/Immunology; Endocrinology

10 mM in DMSO

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

C32H38D3NO2

474.69

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-B1193S/

Isotope-Labeled Compounds

No Development Reported

H1 Receptor