Name: Epinastine HCl
Brand: Selleck Chemicals
SKU: S4253
Availability: InStock
Rating: 5 (1 reviews)

Jump to

Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.45

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Products	GSK2879552 Dihydrochloride JNJ-7777120 Mianserin HCl Ebastine Ciproxifan Maleate Dimethindene maleate Rupatadine Levodropropizine Chloropyramine hydrochloride Lafutidine

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (199.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 57 mg/mL

Ethanol : 57 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	285.77	Formula	C₁₆H₁₅N₃.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	108929-04-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	WAL-801CL HCl			Smiles	C1C2C3=CC=CC=C3CC4=CC=CC=C4N2C(=N1)N.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Histamine receptor
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 K_i 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/2461715/ [2] https://pubmed.ncbi.nlm.nih.gov/9671095/ [3] https://pubmed.ncbi.nlm.nih.gov/1375955/ [4] https://pubmed.ncbi.nlm.nih.gov/9020026/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Epinastine HCl Histamine Receptor inhibitor

Chemical Structure

Molecular Weight: 285.77