Celiprolol hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种心脏选择性 β1 肾上腺素能拮抗剂，具有内在的拟交感神经活性。

A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity.

Celiprolol hydrochloride (0-3 mM, 90 min) is uptaken by human small intestinal transporter OATP-A/1A2 in Xenopus Laevis oocytes.Celiprolol hydrochloride (10 μM, 0-50 min) is transported across human intestinal epithelial (Caco-2) cells by mediation of multiple transporters including P-glycoprotein.

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.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. Animal Model:Type II male Otsuka Long-Evans Tokushima Fatty (OLETF) diabetic rats 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 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.

Corliprol | NSC 324509

Endocrinology/Hormones

Adrenergic Receptor

β-adrenergic receptor

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57470-78-7

415.96

C20H33N3O4·HCl

>98% (HPLC)

DMSO: 10 mM

Cl.CCN(CC)C(=O)NC1=CC(C(C)=O)=C(OCC(O)CNC(C)(C)C)C=C1

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(-20℃)

With Ice Pack

≥ 2 years