Rupatadine (fumarate)

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Cat No: 29478

Biochemicals - Receptor Pharmacology

Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors.{46659} It binds to rabbit platelet membranes and guinea pig cerebellum membranes with apparent Ki values of 0.55 and 0.1 µM, respectively, in radioligand bindi...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

8-chloro-6,11-dihydro-11-[1-[(5-methyl-3-pyridinyl)methyl]-4-piperidinylidene]-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, (2E)-2-butenedioate

Correlated keywords:

158876-82-5 H-1

Product Overview:
Rupatadine is an antagonist of histamine H1 and platelet-activating factor (PAF) receptors.{46659} It binds to rabbit platelet membranes and guinea pig cerebellum membranes with apparent Ki values of 0.55 and 0.1 µM, respectively, in radioligand binding assays. It inhibits contraction of isolated guinea pig ileum induced by histamine (pA2 = 9.29) and platelet aggregation induced by PAF in washed rabbit platelets (pA2 = 6.68). Rupatadine prevents histamine- or PAF-induced hypotension in rats (ID50s = 1.4 and 0.44 mg/kg, respectively) and reverses histamine- or PAF-induced bronchoconstriction in guinea pigs (ID50s = 113 and 9.6 mg/kg, respectively). It does not reduce locomotor activity or potentiate sleep induced by barbiturates in mice, indicating a lack of sedative effects.

Size	50 mg
Shipping	dry ice
CAS Number	182349-12-8
Molecular Formula	C₂₆H₂₆ClN₃ • C₄H₄O₄
SMILES	ClC1=CC=C(/C(C2=NC=CC=C2CC3)=C4CCN(CC5=CN=CC(C)=C5)CC\4)C3=C1.OC(/C=C/C(O)=O)=O
Molecular Weight	532
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
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.