For research use only.
Catalog No.S4253 Synonyms: WAL-801CL HCl
CAS No. 108929-04-0
Epinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||Epinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.|
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. 
|In vivo||Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. |
|In vitro||DMSO||57 mg/mL (199.46 mM)|
|Water||57 mg/mL (199.46 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02260037||Completed||Drug: Epinastine nasal|Drug: Placebo||Healthy||Boehringer Ingelheim||August 2001||Phase 1|
|NCT02182570||Completed||Drug: WAL 801 CL dry syrup||Dermatitis Atopic||Boehringer Ingelheim||June 2001||Phase 3|
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