A histamine H1 receptor antagonist and ERG channel blocker
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Active Metabolite(s)
41828Norastemizole
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Astemizole

Item No. 16967

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
CAS Number
68844-77-9
Synonyms
  • NSC 329963
Molecular Formula
C28H31FN4O
Formula Weight
458.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 5 mg/ml
λmax
215, 250, 285 nm
SMILES
COC1=CC=C(CCN2CCC(NC3=NC4=C(C=CC=C4)N3CC5=CC=C(F)C=C5)CC2)C=C1
InChi Code
InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
InChi Key
GXDALQBWZGODGZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    25 mg

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    Cayman Chemical
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    Product Description

    Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM.1 It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM).2 Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been used to study long QT syndrome type 2.3,4 Furthermore, because it can target oncogenic ERG1 and ERG potassium channels, astemizole has been explored as a potential antineoplastic agent for decreasing proliferation of various cancer cells.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ahn, H.S., and Barnett, A. Selective displacement of [3H]mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamine. Eur. J. Pharmacol. 127(1-2), 153-155 (1986).

    2. Kubo, N., Shirakawa, S., Kuno, T., et al. Antimuscarinic effects of antihistamines: Quantitative evaluation by receptor-binding assay. Jpn. J. Pharmacol. 43(3), 277-282 (1987).

    3. Du, L.P., Tsai, K.C., Li, M.Y., et al. The pharmacophore hypotheses of IKr potassium channel blockers: Novel class III antiarrhythmic agents. Bioorg. Med. Chem. Lett. 14(18), 4771-4777 (2004).

    4. Ficker, E., Obejero-Paz, C.A., Zhao, S., et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. The Journal of Biological Chemisty 277(7), 4989-4998 (2002).

    5. García-Quiroz, J., García-Becerra, R., Santos-Martínez, N., et al. In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumors. BMC Cancer 14, 2-10 (2014).