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Download Product Insert (PDF) PRODUCT INFORMATION Ebastine Item No. 15372 CAS Registry No.: 90729-43-4 Formal Name: 1-[4-(1,1-dimethylethyl)phenyl]- 4-[4-(diphenylmethoxy)-1- piperidinyl]-1-butanone N Synonyms: LAS-W 090, RP 64305 O MF: C32H39NO2 FW: 469.7 O Purity: ≥98% UV/Vis.: λmax: 252 nm Supplied as: A crystalline solid Storage: -20°C Stability: As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly Laboratory Procedures Ebastine is supplied as a crystalline solid. A stock solution may be made by dissolving the ebastine in the solvent of choice. Ebastine is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of ebastine in ethanol and DMSO is approximately 2 mg/ml and approximately 25 mg/ml in DMF. Ebastine is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day. Description Ebastine is a potent second generation histamine H1 receptor antagonist (Ki = 0.4 nM; IC50 = 45 nM) that does not cross the blood brain barrier.1 It undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine, which exerts most of the pharmacological effects.2 At 10 μM, ebastine has been shown to inhibit T cell proliferation and the production of Th2-type pro-inflammatory cytokines by macrophages.3 References 1. Abou-Gharbia, M., Moyer, J.A., Nielsen, S.T., et al. New antihistamines: Substituted piperazine and piperidine derivatives as novel H1-antagonists. J. Med. Chem. 38(20), 4026-4032 (1995). 2. Vincent, J., Liminana, R., Meredith, P.A., et al. The pharmacokinetics, antihistamine and concentration- effect relationship of ebastine in healthy subjects. Br. J. Clin. Pharmacol. 26(5), 497-502 (1988). 3. Nori, M., Iwata, S., Munakata, Y., et al. Ebastine inhibits T cell migration, production of Th2-type cytokines and proinflammatory cytokines. Clin. Exp. Allergy 33(11), 1544-1554 (2003). WARNING CAYMAN CHEMICAL THIS PRODUCT IS FOR RESEARCH ONLY - NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE. 1180 EAST ELLSWORTH RD SAFETY DATA ANN ARBOR, MI 48108 · USA This material should be considered hazardous until further information becomes available. Do not ingest, inhale, get in eyes, on skin, or on clothing. Wash thoroughly after handling. Before use, the user must review the complete Safety Data Sheet, which has been sent via email to your institution. PHONE: [800] 364-9897 WARRANTY AND LIMITATION OF REMEDY [734] 971-3335 Buyer agrees to purchase the material subject to Cayman’s Terms and Conditions. Complete Terms and Conditions including Warranty and Limitation of Liability information can be found on our website. FAX: [734] 971-3640 [email protected] Copyright Cayman Chemical Company, 04/18/2016 WWW.CAYMANCHEM.COM.
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