1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Epinastine

Epinastine (Synonyms: WAL801)

Cat. No.: HY-B0640 Purity: >98.0%
Handling Instructions

Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action.

For research use only. We do not sell to patients.

Epinastine Chemical Structure

Epinastine Chemical Structure

CAS No. : 80012-43-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
Estimated Time of Arrival: December 31
100 mg USD 132 In-stock
Estimated Time of Arrival: December 31
500 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Description

Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

249.31

Formula

C₁₆H₁₅N₃

CAS No.

80012-43-7

SMILES

NC1=NCC2N1C3=CC=CC=C3CC4=CC=CC=C24

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (200.55 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0111 mL 20.0554 mL 40.1107 mL
5 mM 0.8022 mL 4.0111 mL 8.0221 mL
10 mM 0.4011 mL 2.0055 mL 4.0111 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (10.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EpinastineWAL801WAL 801WAL-801Histamine ReceptorAntihistaminevertebrateinsectneuronalantiallergicmastcellInhibitorinhibitorinhibit

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Epinastine
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