Celiprolol hydrochloride
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.98%
- CAS. Nr.: 57470-78-7
- Formel: C20H34ClN3O4
- Molecular Weight:415.95
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Celiprolol hydrochloride
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Biologische Aktivität
Beschreibung
IC50 & Target
[4]|
β adrenergic receptor 0.14-8.3 μM (Ki) |
In Vitro
Celiprolol hydrochloride (0-3 mM, 90 min) is uptaken by human small intestinal transporter OATP-A/1A2 in Xenopus Laevis oocytes[5]. Celiprolol hydrochloride (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.
In Vivo
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.
Chemical Information
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CAS. Nr. 57470-78-7
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Appearance Solid
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Molecular Weight 415.95
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Formel C20H34ClN3O4
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OCC(O)CNC(C)(C)C)C(C(C)=O)=C1)N(CC)CC.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (300.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (120.21 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.4041 mL | 12.0207 mL | 24.0414 mL | 60.1034 mL |
| 5 mM | 0.4808 mL | 2.4041 mL | 4.8083 mL | 12.0207 mL | |
| 10 mM | 0.2404 mL | 1.2021 mL | 2.4041 mL | 6.0103 mL | |
| 15 mM | 0.1603 mL | 0.8014 mL | 1.6028 mL | 4.0069 mL | |
| 20 mM | 0.1202 mL | 0.6010 mL | 1.2021 mL | 3.0052 mL | |
| 25 mM | 0.0962 mL | 0.4808 mL | 0.9617 mL | 2.4041 mL | |
| 30 mM | 0.0801 mL | 0.4007 mL | 0.8014 mL | 2.0034 mL | |
| 40 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5026 mL | |
| 50 mM | 0.0481 mL | 0.2404 mL | 0.4808 mL | 1.2021 mL | |
| 60 mM | 0.0401 mL | 0.2003 mL | 0.4007 mL | 1.0017 mL | |
| 80 mM | 0.0301 mL | 0.1503 mL | 0.3005 mL | 0.7513 mL | |
| 100 mM | 0.0240 mL | 0.1202 mL | 0.2404 mL | 0.6010 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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