Description
CGP48369 is a nonpeptidic angiotensin II receptor antagonist, used for anti-hypertensive research.
Product information
CAS Number: 135689-23-5
Molecular Weight: 442.56
Formula: C26H30N6O
Chemical Name: 2,6-dibutyl-5-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-3,4-dihydropyrimidin-4-one
Smiles: CCCCC1N=C(CCCC)NC(=O)C=1CC1C=CC(=CC=1)C1=CC=CC=C1C1NN=NN=1
InChiKey: UKEZYWUWLICNPR-UHFFFAOYSA-N
InChi: InChI=1S/C26H30N6O/c1-3-5-11-23-22(26(33)28-24(27-23)12-6-4-2)17-18-13-15-19(16-14-18)20-9-7-8-10-21(20)25-29-31-32-30-25/h7-10,13-16H,3-6,11-12,17H2,1-2H3,(H,27,28,33)(H,29,30,31,32)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CGP 48369 binds to the ATl receptor (IC50 1.8 nM in vascular smooth musc1e cells, VSMC) and inhibits AII-induced contraction in rabbit aorta (IC50 8.7 nM).
In Vivo:
CGP48369 (10 mg/kg/day p.o.) decreases BP in two-kidney/one-clip renal hypertensive rats for at least 24 h. In arteries with endothelium, contractions induced by AII 3×10-8 M do not differ in untreated spontaneously hypertensive rats (SHR) and WKY. All evoked significantly smaller contractions in SHR treated with CGP 48369 than in the other treated SHR. Antihypertensive treatment with benazepril or nifedipine, and to a lesser extent with CGP 48369, increases the sensitivity (pD2-va1ue) to intraluminal ACh. In arteries without endothelium, sensitivity to NE is identical in all groups, whereas maximal response in CGP 48369-treated SHR and in nifedipine treated SHR is slightly greater as compared with that in WKY. In SHR, antihypertensive therapy with either benazepril HCl, CGP 48369, valsartan, or nifedipine (each 10 mg/kg/d for 8 weeks) significantly increase endothelium-dependent relaxations evoked by acetylcholine.
Products are for research use only. Not for human use.
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