Epinastine hydrochloride

SKU: orb1300724

Description

Epinastine hydrochloride (WAL-801CL HCl) is a dual-action small molecule antagonist of the histamine H1 receptor and a mast cell stabilizer. It is widely used in ophthalmic solutions for allergic conjunctivitis and serves as a key research tool for investigating allergic mechanisms in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 108929-04-0
• MW: 285.77
• Purity: 99.92% (May vary between batches)
• Formula: C₁₆H₁₅N₃·HCl
• SMILES: Cl[H].NC1=NCC2N1C1=CC=CC=C1CC1=CC=CC=C21
• Target: 5-HT Receptor,Interleukin,Histamine Receptor
• Solubility: Ethanol:53 mg/mL (185.46 mM);DMSO:50 mg/mL (174.97 mM);H2O:52 mg/mL (181.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7 mM)

Bioactivity

• In Vivo:
  Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs.
• In Vitro:
  Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain. Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

antiallergic, Antihistamine, 5HT Receptor, 5HTReceptor, Alesion, cell, inhibit, neuronal, mast, Histamine Receptor, HistamineReceptor, Inhibitor, insect, Epinastine, Epinastine HCl, Epinastine Hydrochloride, Epinastine hydrochloride, Elestat, HT, WAL 801, WAL-801CL HCl, WAL801, WAL-801, vertebrate

Compound Identifiers

PubChem CID

157313