Alcaftadine, a imidazobenzazepine-based antagonist of the histamine receptors, has a pKi of 8.5 and 5.8 for the H1 receptor and H4 receptors, respectively. Additionally, Alcaftadine shows higher affinity for the H2 receptor than ketotifen. [1]In support of its potent anti-inflammatory properties, Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects. [2] Receptor binding studies revealed less significant effects ranging from a moderate affinity for cholinergic muscarinic receptors and lower affinity for human a2A-adrenoreceptors, serotonin 5-H51A, 5-HT2A receptors, and melanocortin MC4 receptors. [2] Furthermore, displacement experiments showed that at concentrations up to 10 uM, Alcaftadine did not interact with other receptors, transporters, or ion channel binding sites, including the hERG channel. [3]
Technical information:
| Chemical Formula: | C19H21N3O | |
| CAS #: | 147084-10-4 | |
| Molecular Weight: | 307.38 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde | |
| Solubility: | Up to 20 mM in DMSO | |
| Synonyms: | Alcaftadine, 147084-10-4, Lastacaft |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Gallois-Bernois et al., Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1, H2, and H4 receptors. J. Receptor Ligand Channel Res. 2012, 5, 9-20. |
| 2. | Namdar et al., Alcaftadine: A topical antihistamine for use in allergic conjunctivitis. Drugs of Today, 2011, 47(12), 883-890. Pubmed ID:22348913 |
| 3. | Bohets et al., Clinical Pharmacology of Alcaftadine, a Novel Antihistamine for the Prevention of Allergic Conjunctivitis. J. Ocular. Pharm. Ther. 2011, 27(2), 187-195. |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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