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Astemizole

CAT: 0804-HY-12532-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12532-01Size:5 mg
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Description
Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2].
CAS Number
68844-77-9
Product Name Alternative
R 43512
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Histamine Receptor; Potassium Channel
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology; Endocrinology
Assay Protocol
https://www.medchemexpress.com/astemizole.html
Purity
99.77
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1
Molecular Formula
C28H31FN4O
Molecular Weight
458.57
Precautions
H302, H315, H319, H335
References & Citations
[1]Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21 (2) :294-300.|[2]Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28 (1) :38-61.|[3]Ikuo Horii, et al. Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine. J Toxicol Sci. 2002 May;27 (2) :123-30.|[4]Hiroko Izumi-Nakaseko, et al. Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. J Pharmacol Sci. 2016 Jun;131 (2) :150-3.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
H1 Receptor

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CatalogName
T1278-01Astemizole

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