Cat. No.: HY-B1264

Celiprolol hydrochloride

1 Cited Publications

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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 K_i 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.

For research use only. We do not sell to patients.

Purity: 99.98%
CAS No.: 57470-78-7
Formula: C₂₀H₃₄ClN₃O₄
Molecular Weight:415.95

Storage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Celiprolol hydrochloride Chemical Structure

CAS No.: 57470-78-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[4]

β adrenergic receptor

0.14-8.3 μM (Ki)

All NO Synthase Isoforms :

All Adrenergic Receptor Isoforms :

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

Celiprolol hydrochloride (Oral administration, 100 mg/kg/day for 31 days) improves endothelial function in the arteries of in Otsuka Long-Evans Tokushima Fatty (OLETF) rats, and restores it 4 weeks after endothelial denudation in the arteries of OLETF rats^[2].
Celiprolol hydrochloride (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.

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.

Chemical Information

CAS No. 57470-78-7
Appearance Solid
Molecular Weight 415.95
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

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

Solvent & Solubility

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4041 mL

12.0207 mL

24.0414 mL

5 mM

0.4808 mL

2.4041 mL

4.8083 mL

10 mM

0.2404 mL

1.2021 mL

2.4041 mL

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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

1 Cited Publications

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Celiprolol hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Celiprolol hydrochloride

All NO Synthase Isoforms

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Celiprolol hydrochloride Related Classifications

HY-B1264 Related Classifications