Epinastine (hydrochloride)

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Cat No: 18136

Biochemicals - Receptor Pharmacology

Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cor...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3-amine, monohydrochloride

Correlated keywords:

80012-43-7 allergy inflammation antihistamine antagonist H1 receptor mast cell stabilizer anti-histamine biochemical elestat alesion WAL801CL WAL801-CL WAL-801-CL

Product Overview:
Epinastine is a histamine H1 receptor antagonist (Kiapps = 1.41 and 1.62 nM using guinea pig cerebellar and lung membranes, respectively) and mast cell stabilizer.{48871,48872} It inhibits IgE-induced histamine, TNF-α, and IL-10 secretion in human cord blood stem cell-derived mast cells (CBMCs) when used at a concentration of 0.1 μg/ml.{48872} Epinastine inhibits histamine-induced cutaneous vascular permeability in rats and bronchoconstriction in anesthetized guinea pigs (ID50s = 5 and 0.1 mg/kg, respectively).{11338} It inhibits dye leakage into the conjunctiva in a rat model of passive anaphylaxis reaction-induced vascular hyperpermeability of the conjunctiva (ID50 = 9.7 mg/kg, p.o.).{48873} Topical administration of formulations containing epinastine (0.05% three times per day) reduces lid edema, tearing, and redness, as well as the number of neutrophils and eosinophils in the lid fornix, in a mouse model of atopic conjunctivitis.{48872} Formulations containing epinastine have been used in the prevention of itching associated with allergic conjunctivitis.

Size	10 mg
Shipping	dry ice
CAS Number	108929-04-0
Molecular Formula	C₁₆H₁₅N₃ • HCl
SMILES	NC1=NCC2C(C=CC=C3)=C3CC(C=CC=C4)=C4N21.Cl
Molecular Weight	285,8
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.