1. Immunology/Inflammation
    Neuronal Signaling
    GPCR/G Protein
  2. NO Synthase
    Adrenergic Receptor
  3. Celiprolol hydrochloride

Celiprolol hydrochloride 

Cat. No.: HY-B1264
Handling Instructions

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.

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

Celiprolol hydrochloride Chemical Structure

Celiprolol hydrochloride Chemical Structure

CAS No. : 57470-78-7

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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].

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].

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].

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.
Clinical Trial
Molecular Weight

415.95

Formula

C20H34ClN3O4

CAS No.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Celiprolol hydrochloride
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HY-B1264
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