Art. -Nr.: HY-B0640

Epinastine

(Synonyms: WAL801)

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Epinastine (WAL801) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine has high affinity for neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine can be used in the research of allergic diseases.

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Reinheit: 98.0%
CAS. Nr.: 80012-43-7
Formel: C₁₆H₁₅N₃
Molecular Weight:249.32

Speicherung:

4°C, protect from light, stored under nitrogen

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

Epinastine Chemical Structure

CAS. Nr.: 80012-43-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]

H₁ Receptor

IL-8

IL-4

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	1.1 μM Compound: epinastine	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	29.8 μM Compound: epinastine	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
HEK293	IC₅₀	4.3 μM Compound: epinastine	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	[PMID: 23241029]

In Vitro

Epinastine (50-100 μM) inhibits histamine release from rat peritoneal mast cells induced by antigen-antibody reaction^[1].
Epinastine shows high affinity for neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM), specifically displaces [³H]NC-5Z binding to these receptors^[2].
Epinastine (1-25 μg/mL; 3-24 h) dose- and time-dependently suppresses constitutive and Calcium ionophore-induced IL-8 release from human eosinophils of atopic patients^[3].
Epinastine (1 μM; preincubation for 15 min, then incubation for 19 h) tends to inhibit PHA (HY-N7038)-induced IL-4 mRNA expression in peripheral blood mononuclear cells (PBMC) from asthmatic patients^[4].
Epinastine (0.1 μM - 10 μM; 24 h) inhibits IgE secretion from rat IgE-producing hybridoma FE-3 cells^[5].

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

Real Time qPCR^[4]

Cell Line:

Human peripheral blood mononuclear cells (PBMC) from asthmatic patients
Concentration:

1 μM
Incubation Time:

15 min (preincubation) + 19 h (incubation with PHA/HDM)
Result:

Tended to inhibit PHA-induced IL-4 mRNA expression (1.26 vs 0.74).
Had no significant effect on HDM-induced IL-4 mRNA expression.

In Vivo

Epinastine (1-30 mg/kg; p.o.; 60 min before stimulation) inhibits Substance P (HY-P0201)-induced scratching behavior and vascular permeability increase in ddY mice, but does not affect Dinitrofluorobenzene-induced scratching behavior in BALB/c mice^[7].
Epinastine (2-6 mg/kg; i.p.; 14 days) significantly inhibits tumor growth in C57BL/6N mice bearing MC38 tumors, enhances infiltration and IFN-γ secretion of CD8⁺ T cells and NK cells in tumor tissues, and has no toxicity to major organs^[8].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 80012-43-7
Appearance Solid
Molecular Weight 249.32
Formel C₁₆H₁₅N₃
Color White to off-white
SMILES

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

WAL801
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (200.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0110 mL

20.0548 mL

40.1096 mL

5 mM

0.8022 mL

4.0110 mL

8.0219 mL

10 mM

0.4011 mL

2.0055 mL

4.0110 mL

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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. C Kamei, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205. [Content Brief]

[2]. T Roeder, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. ur J Pharmacol. 1998 May 22;349(2-3):171-7. [Content Brief]

[3]. T Kohyama, et al. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8. [Content Brief]

[4]. Nakagawa T, et al. Modulatory effects of epinastine hydrochloride on IL-4 mRNA expression by peripheral blood mononuclear cells. Int Arch Allergy Immunol. 1997 May-Jul;113(1-3):321-2. [Content Brief]

[5]. Hanashiro K, et al. Antiallergic drugs, azelastine hydrochloride and epinastine hydrochloride, inhibit ongoing IgE secretion of rat IgE-producing hybridoma FE-3 cells. Eur J Pharmacol. 2006 Oct 10;547(1-3):174-83. [Content Brief]

[6]. Kanai K, et al. Suppressive activity of epinastine hydrochloride on TARC production from human peripheral blood CD4+ T cells in-vitro. J Pharm Pharmacol. 2005 Aug;57(8):1027-36. [Content Brief]

[7]. Inagaki N, et al. Evaluation of anti-scratch properties of oxatomide and epinastine in mice. Eur J Pharmacol. 2000 Jul 14;400(1):73-9. [Content Brief]

[8]. Zhang X, et al. Identification of Epinastine as CD96/PVR inhibitor for cancer immunotherapy. BMC Biol. 2025 Jan 27;23(1):27. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0110 mL	20.0548 mL	40.1096 mL	100.2739 mL
	5 mM	0.8022 mL	4.0110 mL	8.0219 mL	20.0548 mL
	10 mM	0.4011 mL	2.0055 mL	4.0110 mL	10.0274 mL
	15 mM	0.2674 mL	1.3370 mL	2.6740 mL	6.6849 mL
	20 mM	0.2005 mL	1.0027 mL	2.0055 mL	5.0137 mL
	25 mM	0.1604 mL	0.8022 mL	1.6044 mL	4.0110 mL
	30 mM	0.1337 mL	0.6685 mL	1.3370 mL	3.3425 mL
	40 mM	0.1003 mL	0.5014 mL	1.0027 mL	2.5068 mL
	50 mM	0.0802 mL	0.4011 mL	0.8022 mL	2.0055 mL
	60 mM	0.0668 mL	0.3342 mL	0.6685 mL	1.6712 mL
	80 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2534 mL
	100 mM	0.0401 mL	0.2005 mL	0.4011 mL	1.0027 mL

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Epinastine

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Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Epinastine Related Classifications

HY-B0640 Related Classifications