80012-43-7
Chemical Structure
Epinastine
Synonym(s): WAL801
- CAS No.: 80012-43-7
- Formula:C16H15N3
- Molecular Weight:249.32
IUPAC Name: 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine
InChIKey: WHWZLSFABNNENI-UHFFFAOYSA-N
SMILES: NC1=NCC2N1C3=CC=CC=C3CC4=CC=CC=C24
Biological Activity: 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 (HY-P0201)-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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Epinastine | 98.0% | 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 (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine can be used in the research of allergic diseases. | ||||||||||||||||||||
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Epinastine-13C,d3 hydrobromide | Epinastine-13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. 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. | |||||||||||||||||||||
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References
- [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]
