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Astemizole
$50 – $260
Products Details
Product 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].
Web ID
– HY-12532
Storage Temperature
– -20°C, 3 years (Powder)
Shipping
– Blue Ice
Applications
– COVID-19-immunoregulation
Molecular Formula
– C28H31FN4O
References
– [1]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.|[2]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.|[3]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.|[4]Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61.
CAS Number
– 68844-77-9
Molecular Weight
– 458.57
Compound Purity
– 99.68
SMILES
– COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1
Clinical Information
– Launched
Research Area
– Inflammation/Immunology; Endocrinology
Solubility
– DMSO : 125 mg/mL (ultrasonic)
Target
– Histamine Receptor;Potassium Channel
Isoform
– H1 Receptor
Pathway
– GPCR/G Protein;Immunology/Inflammation;Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
