1. Celiprolol hydrochloride

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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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].

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.
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

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Purity & Documentation
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  • 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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