A histamine H1 receptor antagonist and ERG channel blocker
Related Products
Active Metabolite(s)
41828Norastemizole
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    25 mg

    $54

    Add

    50 mg

    $102

    Add

    100 mg

    $190

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    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).