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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.98%
- CAS 番号: 57470-78-7
- 分子式: C20H34ClN3O4
- 分子量:415.95
-
保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Celiprolol hydrochloride
MoreAdrenergic Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
[4]|
β adrenergic receptor 0.14-8.3 μM (Ki) |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Type II male Otsuka Long-Evans Tokushima Fatty (OLETF) diabetic rats[2]
-
Dosage:100 mg/kg/day for 31 days
-
Administration:Oral administration
-
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.
-
Animal Model:Deoxycorticosterone acetate (DOCA)-salt hypertensive rats [3]
-
Dosage:10 mg/kg/d for 5 weeks
-
Administration:Treated in drinking water
-
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.
化学情報
-
CAS 番号 57470-78-7
-
性状 Solid
-
分子量 415.95
-
分子式 C20H34ClN3O4
-
Color White to off-white
-
SMILES
O=C(NC1=CC=C(OCC(O)CNC(C)(C)C)C(C(C)=O)=C1)N(CC)CC.[H]Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (277 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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.
Celiprolol hydrochloride 関連分類
HY-B1264 関連分類
Powered by Bioz