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CGP48369

Catalog No. T14942 CAS 135689-23-5

CGP48369 is a potent angiotensin II receptor antagonist with antihypertensive effects that enhances endothelium-dependent relaxation of coronary arteries in spontaneously hypertensive rats.

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CGP48369, CAS 135689-23-5

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1 mg	In stock	$ 700.00
5 mg	In stock	$ 1,800.00

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Purity: 99.27%

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Description	CGP48369 is a potent angiotensin II receptor antagonist with antihypertensive effects that enhances endothelium-dependent relaxation of coronary arteries in spontaneously hypertensive rats.
Targets&IC50	VSMC cells:1.8 nM
In vitro	Binding to the AT1 receptor (IC50 1.8 nM in vascular smooth muscle cells, VSMC), CGP 48369 inhibits AII-induced contraction in rabbit aorta (IC50 8.7 nM)[2].
In vivo	In two-kidney/one-clip renal hypertensive rats, CGP48369 (10 mg/kg/day p.o.) reduces blood pressure for at least 24 h. In arteries with endothelium, contractions induced by AII at 3×10-8 M do not differ between untreated spontaneously hypertensive rats (SHR) and Wistar-Kyoto (WKY) rats. However, significantly smaller contractions are observed in SHR treated with CGP48369 compared to the other treated SHR groups. Antihypertensive treatment with benazepril or nifedipine, and to a lesser extent with CGP48369, increases sensitivity (pD2-value) to intraluminal ACh. In arteries without endothelium, sensitivity to NE is identical in all groups, while the maximal response in CGP48369-treated SHR and nifedipine-treated SHR is slightly greater compared to that in WKY[1]. In SHR, antihypertensive therapy with benazepril HCl, CGP48369, valsartan, or nifedipine (each 10 mg/kg/day for 8 weeks) significantly increases endothelium-dependent relaxations evoked by acetylcholine[1].

Molecular Weight	442.56
Formula	C26H30N6O
CAS No.	135689-23-5

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store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Tschudi MR, et al. Antihypertensive therapy augments endothelium-dependent relaxations in coronary arteries of spontaneously hypertensive rats. Circulation. 1994 May;89(5):2212-8. 2. Dohi Y, et al. Angiotensin blockade or calcium antagonists improve endothelial dysfunction in hypertension: studies in perfused mesenteric resistance arteries. J Cardiovasc Pharmacol. 1994 Sep;24(3):372-9.

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Keywords

CGP48369 135689-23-5 Endocrinology/Hormones RAAS CGP-48369 CGP 48369 inhibitor inhibit

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