Home Neuronal Signaling Histamine Receptor inhibitor Epinastine HCl For research use only.

Epinastine HCl

Synonyms: WAL-801CL HCl

Epinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

Epinastine HCl Chemical Structure

Epinastine HCl Chemical Structure

CAS: 108929-04-0

Purity & Quality Control

Batch: S425301 DMSO] 57 mg/mL] false] Water] 57 mg/mL] false] Ethanol] 57 mg/mL] false Purity: 99.45%
99.45

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Biological Activity

Description Epinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
Targets
Histamine receptor [1]
In vitro
In vitro Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. [1] 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. [2] 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. [3] 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. [4]
In Vivo
In vivo Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02260037 Completed Healthy Boehringer Ingelheim August 2001 Phase 1
NCT02182570 Completed Dermatitis Atopic Boehringer Ingelheim June 2001 Phase 3

Chemical lnformation & Solubility

Molecular Weight 285.77 Formula

C16H15N3.HCl
CAS No. 108929-04-0 SDF Download Epinastine HCl SDF
Smiles C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (199.46 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 57 mg/mL

Ethanol : 57 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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