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Product Description
– Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure[1][4].
Web ID
– HY-B1264
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C20H34ClN3O4
References
– [1]James J Nawarskas, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253. |[2]Toshio Hayashi, et al. beta1 antagonist and beta2 agonist, celiprolol, restores the impaired endothelial dependent and independent responses and decreased TNFalpha in rat with type II diabetes. Life Sci. 2007 Jan 16;80(6):592-9. |[3]Naohiko Kobayashi, et al. Celiprolol activates eNOS through the PI3K-Akt pathway and inhibits VCAM-1 Via NF-kappaB induced by oxidative stress. Hypertension. 2003 Nov;42(5):1004-13. |[4]R G Van Inwegen, et al. Effects of celiprolol (REV 5320), a new cardioselective beta-adrenoceptor antagonist, on in vitro adenylate cyclase, alpha- and beta-adrenergic receptor binding and lipolysis. Arch Int Pharmacodyn Ther. 1984 Nov;272(1):40-55. |[5]Yukio Kato, et al. Involvement of influx and efflux transport systems in gastrointestinal absorption of celiprolol. J Pharm Sci. 2009 Jul;98(7):2529-39. |[6]J. Karlsson, et al. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br J Pharmacol. 1993 Nov; 110(3): 1009–1016.
CAS Number
– 57470-78-7
Molecular Weight
– 415.95
SMILES
– O=C(NC1=CC=C(OCC(O)CNC(C)(C)C)C(C(C)=O)=C1)N(CC)CC.[H]Cl
Clinical Information
– Launched
Research Area
– Cardiovascular Disease
Solubility
– 10 mM in DMSO
Target
– Adrenergic Receptor;NO Synthase
Isoform
– β adrenergic receptor
Pathway
– GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling
Product type
– Reference compound
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