Celiprolol
Based on 1 publication(s) in Google Scholar
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.
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- CAS No.: 56980-93-9
- Formule: C20H33N3O4
- Masse moléculaire:379.49
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Celiprolol
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Activité biologique
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β adrenergic receptor 0.14-8.3 μM (Ki) |
Celiprolol (0-3 mM, 90 min) is uptaken by human small intestinal transporter OATP-A/1A2 in Xenopus Laevis oocytes[5].
Celiprolol (10 μM, 0-50 min) is transported across human intestinal epithelial (Caco-2) cells by mediation of multiple transporters including P-glycoprotein[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Celiprolol (Treated in drinking water, 10 mg/kg/day for 5 weeks) suppresses VCAM-1 expression by inhibition of oxidative stress, NF-κB, signal transduction, and increases eNOS via stimulation of the PI3K-Akt pathway, and improves cardiovascular remodeling in deoxycorticosterone acetate (DOCA)-salt hypertensive rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Type II male Otsuka Long-Evans Tokushima Fatty (OLETF) diabetic rats[2]
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Dosage:100 mg/kg/day for 31 days
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Administration:Oral administration
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Result:Improved acetylcholine-induced NO-dependent relaxation in arteries. Improved tone-related basal NO release and acetylcholine-induced NO-dependent relaxation in the arteries and plasma NOx.
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Animal Model:Deoxycorticosterone acetate (DOCA)-salt hypertensive rats [3]
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Dosage:10 mg/kg/d for 5 weeks
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Administration:Treated in drinking water
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Result:Activated phosphorylation of eNOS through the PI3K-Akt signaling pathway. Modulated VCAM-1 expression, which is associated with inhibition of NF-κB phosphorylation. Reduced production of ROS by suppressing NAD(P)H oxidase subunit p22phox, p47phox, gp91phox, and nox1 expression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 56980-93-9
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Masse moléculaire 379.49
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Formule C20H33N3O4
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SMILES
O=C(N(CC)CC)NC1=CC=C(C(C(C)=O)=C1)OCC(CNC(C)(C)C)O
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Synonyms
REV 5320
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569
Pureté et documentation
Références
[1]. James J Nawarskas, et, al. Celiprolol: A Unique Selective Adrenoceptor Modulator. Cardiol Rev. Sep/Oct 2017; 25(5): 247-253. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Celiprolol Related Classifications
HY-119873 Related Classifications
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