Desmethylastemizole

Desmethylastemizole (O-Demethylastemizole), a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06 μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K+ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research[1][2][3].

Product Specifications

CAS Number

[73736-50-2]

Product Name Alternative

O-Demethylastemizole

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Drug Metabolite; Histamine Receptor; Parasite; Potassium Channel

Related Pathways

Anti-infection; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Field of Research

Infection; Cardiovascular Disease

Purity

98.26

Smiles

FC(C=C1)=CC=C1CN2C3=CC=CC=C3N=C2NC4CCN(CCC5=CC=C(O)C=C5)CC4

Molecular Formula

C27H29FN4O

Molecular Weight

444.54

Precautions

H302, H315, H319, H335

References & Citations

[1]Kamei C, Mio M, Izushi K, et al. Antiallergic effects of major metabolites of astemizole in rats and guinea pigs. Arzneimittelforschung. 1991;41 (9) :932-936.|[2]Kumar M, Okombo J, Mambwe D, et al. Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action. ACS Infect Dis. 2019;5 (2) :303-315. |[3]Zhou Z, et al. Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10 (6) :836-43.