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.
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- CAS. Nr.: 73736-50-2
- Formel: C27H29FN4O
- Molecular Weight:444.54
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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H1 Receptor |
Plasmodium falciparum sporozoites |
Chemical Information
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CAS. Nr. 73736-50-2
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Appearance Solid
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Molecular Weight 444.54
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Formel C27H29FN4O
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Color White to off-white
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SMILES
FC(C=C1)=CC=C1CN2C3=CC=CC=C3N=C2NC4CCN(CCC5=CC=C(O)C=C5)CC4
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Synonyms
O-Demethylastemizole
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Desmethylastemizole Related Classifications
HY-W516880 Related Classifications
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