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编 号：F394510
分子式：C20H34ClN3O4
分子量：415.95
分子式：C20H34ClN3O4
分子量：415.95
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CAS No: 57470-78-7
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 (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.
体内研究：
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.
体外研究：
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.
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