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

Emedastine 

Cat. No.: HY-108411 Purity: >98.0%
Handling Instructions

Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

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

Emedastine Chemical Structure

Emedastine Chemical Structure

CAS No. : 87233-61-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].

IC50 & Target[1]

H1 Receptor

1.3 nM (Ki)

H2 Receptor

49067 nM (Ki)

H3 Receptor

12430 nM (Ki)

In Vitro

Emedastine inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1].
High concentrations of Emedastine (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2].
Emedastine (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].

In Vivo

Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3].
Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3].
Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2].
Emedastine inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2].

Animal Model: Male ICR mice 5-6 weeks of age[3]
Dosage: 0.03, 0.1, 0.3 mg/kg
Administration: Orally; 30 min before pruritogen injection
Result: Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
Molecular Weight

302.41

Formula

C₁₇H₂₆N₄O

CAS No.

87233-61-2

SMILES

CN1CCN(C2=NC3=CC=CC=C3N2CCOCC)CCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (413.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3068 mL 16.5338 mL 33.0677 mL
5 mM 0.6614 mL 3.3068 mL 6.6135 mL
10 mM 0.3307 mL 1.6534 mL 3.3068 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: ≥ 2.08 mg/mL (6.88 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution

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

EmedastineHistamine ReceptororallybenzimidazoleantiallergicallergicrhinitisskindiseasesconjunctivitisInhibitorinhibitorinhibit

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Emedastine
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HY-108411
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