Astemizole

Catalog No.: A13899

H1-receptor antagonist

Astemizole Chemical Structure

CAS NO. 68844-77-9

Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.

Availability: In stock

Package Price Qty
100 mg
$140.00
500 mg
$420.00
Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.

Biological Activity

Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 21.81 mL 109.03 mL 218.07 mL
0.5 mM 4.36 mL 21.81 mL 43.61 mL
1 mM 2.18 mL 10.9 mL 21.81 mL
5 mM 0.44 mL 2.18 mL 4.36 mL

*The above data is based on the productmolecular weight 458.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Catalog Num A13899
Actions Antagonist
M. Wt 458.57
Formula C28H31FN4O
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 68844-77-9
Synonyms Astemisan, Hismanal, Histamen, Paralergim
SMILES COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F

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