An H1 receptor antagonist
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Alcaftadine

Item No. 21290

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b][3]benzazepine-3-carboxaldehyde
CAS Number
147084-10-4
Synonyms
  • R-89674
Molecular Formula
C19H21N3O
Formula Weight
307.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
284 nm
SMILES
O=CC1=CN=C2N1CCC(C=CC=C3)=C3/C2=C4CCN(C)CC\4
InChi Code
InChI=1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
InChi Key
MWTBKTRZPHJQLH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $49

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    10 mg

    $93

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    25 mg

    $190

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    50 mg

    $329

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    Cayman Chemical
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    Product Description

    Alcaftadine is a potent antagonist of the H1 histamine receptor (IC50 = 8.6 nM) with lower affinities for the H2 and H4 receptors (IC50s = 62 nM and 4.4 μM, respectively).1 This antiallergenic agent has anti-inflammatory and mast cell stabilizing effects.2 Alcaftadine has been shown to reduce edema and erythema in a guinea pig model of allergic conjunctivitis (ED50 = 0.1 mg/kg) more effectively than ketotifen (Item No. 20303) (ED50 = 1.0 mg/kg) and has been used in clinical formulations in eye drops for treatment of ocular itching associated with allergic conjunctivitis.1,3 Alcaftadine also binds to 5-HT2A and 5-HT2C receptors (Kis = 2.5 and 1.5 μM, respectively).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gallois-Bernos, A.C., and Thurmond, R.L. Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1, H2, and H4 receptors. J. Receptor Ligand Channel Res. 5, 9-20 (2012).

    2. Ackerman, S., Smith, L.M., and Gomes, P.J. Ocular itch associated with allergic conjunctivitis: Latest evidence and clinical management. Ther. Adv. Chronic Dis. 7(1), 52-67 (2016).

    3. Mahvan, T.D., Buckley, W.A., and Hornecker, J.R. Alcaftadine for the prevention of itching associated with allergic conjunctivitis. Ann. Pharmacother. 46, 1025-1032 (2012).