Epinastine

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 (Ki = 2 nM) and honeybees (Ki = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine activates anti-colon cancer immunity and inhibits Substance P -induced scratching behavior and increased vascular permeability. Epinastine can be used in the research of allergic diseases[1][2][3][4][5][6][7][8].

80012-43-7

WAL801

12352005

H302, H319, H372, H410

Histamine Receptor; Interleukin Related; Transmembrane Glycoprotein

Reference compound

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

COVID-19-immunoregulation

Cancer; Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

https://www.medchemexpress.com/epinastine.html

98.0

DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL (ultrasonic)

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

C16H15N3

249.32

H302, H319, H372, H410

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

Room Temperature

4°C (Powder, protect from light, stored under nitrogen)

Reference compound1

Launched