Emedastine (fumarate)

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Cat No: 23946

Biochemicals - Receptor Pharmacology

Emedastine is a histamine H1 receptor antagonist (Ki = 1.3 nM).{38529} It is selective for histamine H1 over H2 and H3 receptors (Kis = 49 and 12.43 µM, respectively), as well as α1-, α2-, and β1-adrenergic and dopamine D1 and D2 receptors, and the se...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole, 2E-butenedioate (1:2)

Correlated keywords:

87233-61-2 Emadine LY-188695 Rapimine KB-2413 KG-2413 KG2413 5HT1 5HT2 IL6 IL8 GMCSF AL3432A KB2413 interleukin

Product Overview:
Emedastine is a histamine H1 receptor antagonist (Ki = 1.3 nM).{38529} It is selective for histamine H1 over H2 and H3 receptors (Kis = 49 and 12.43 µM, respectively), as well as α1-, α2-, and β1-adrenergic and dopamine D1 and D2 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1 and 5-HT2 at 10 µM.{38529,38530} Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively).{38531} It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC50s = 2.23, 3.42, and 1.50 nM, respectively).{38532} Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs.{38530} Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.

Size	5 mg
Shipping	dry ice
CAS Number	87233-62-3
Molecular Formula	C₁₇H₂₆N₄O • 2C₄H₄O₄
SMILES	CN(CC1)CCCN1C2=NC3=CC=CC=C3N2CCOCC.OC(/C=C/C(O)=O)=O.OC(/C=C\C(O)=O)=O
Molecular Weight	534,6
Formulation	A solid
Purity	≥98%
Custom Code	2921.30
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.