| Cat.No. | Name | Information |
|---|---|---|
| M5393 | Alcaftadine | Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor. |
| M5284 | Lodoxamide tromethamine | Lodoxamide tromethamine is a new drug intended for the prophylaxis of mast cell-mediated allergic disease. |
| M3754 | Nedocromil | Nedocromil is a pyranoquinolone derivative that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. |
| M3665 | Promethazine hydrochloride | Promethazine hydrochloride is a potent histamine H1 receptor antagonist used as a sedative and antiallergic compound. |
| M3487 | Azelastine hydrochloride | Azelastine hydrochloride is a potent, second-generation, selective, histamine antagonist. |
| M3458 | Chlorpheniramine Maleate | Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM. |
| M3454 | Olopatadine hydrochloride | Olopatadine hydrochloride is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine. It can be used in studies related to allergic conjunctivitis and rhinitis. |
| M3431 | Nizatidine | Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM. |
| M3385 | Cimetidine | Cimetidine, a histamine congener, competitively inhibits histamine binding to histamine H2 receptors. |
| M3383 | Diphenhydramine hydrochloride | Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB). |
| M3318 | Clemastine Fumarate | Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. |
| M3226 | Brompheniramine maleate | Brompheniramine maleate is an orally active and selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. |
| M3213 | Meclizine dihydrochloride | Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR. Phase2. |
| M3091 | Tripelennamine hydrochloride | Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM. |
| M2990 | Rupatadine Fumarate | Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. |
| M2971 | Pyrilamine Maleate | Pyrilamine is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. |
| M2935 | Pheniramine Maleate | Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. |
| M2919 | Pemirolast potassium | Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. |
| M2811 | Levodropropizine | Levodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex. |
| M2784 | JNJ-7777120 | JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors. |
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