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

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.

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Emedastine Chemical Structure

Emedastine Chemical Structure

CAS No. : 87233-61-2

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Solid or liquid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
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10 mg USD 145 In-stock
25 mg USD 240 In-stock
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Based on 1 publication(s) in Google Scholar

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Emedastine Related Antibodies

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  • Purity & Documentation

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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].

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

Emedastine Related Antibodies
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].

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

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.
Clinical Trial
Molecular Weight

302.41

Formula

C17H26N4O
CAS No.
Appearance

Viscous Liquid

Color

Yellow to brown

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (330.68 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.01%

COA (250 KB) HNMR (271 KB) RP-HPLC (244 KB) MS (68 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.3068 mL 16.5338 mL 33.0677 mL 82.6692 mL
5 mM 0.6614 mL 3.3068 mL 6.6135 mL 16.5338 mL
10 mM 0.3307 mL 1.6534 mL 3.3068 mL 8.2669 mL
15 mM 0.2205 mL 1.1023 mL 2.2045 mL 5.5113 mL
20 mM 0.1653 mL 0.8267 mL 1.6534 mL 4.1335 mL
25 mM 0.1323 mL 0.6614 mL 1.3227 mL 3.3068 mL
30 mM 0.1102 mL 0.5511 mL 1.1023 mL 2.7556 mL
40 mM 0.0827 mL 0.4133 mL 0.8267 mL 2.0667 mL
50 mM 0.0661 mL 0.3307 mL 0.6614 mL 1.6534 mL
60 mM 0.0551 mL 0.2756 mL 0.5511 mL 1.3778 mL
80 mM 0.0413 mL 0.2067 mL 0.4133 mL 1.0334 mL
100 mM 0.0331 mL 0.1653 mL 0.3307 mL 0.8267 mL
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Emedastine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Emedastine87233-61-2Histamine ReceptororallybenzimidazoleantiallergicallergicrhinitisskindiseasesconjunctivitisInhibitorinhibitorinhibit

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