AVE 0991, Inhibitor | AVE0991, inhibitor

AVE 0991

Cat. Num. AAA5764315

• Purity: 98.00%
• Synonyms: AVE 0991; AVE0991; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (172.20mM); Water: Insoluble; (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C29H32N4O5S2
• SMILES: CCNC(NS(c(sc(CC(C)C)c1)c1-c1ccc(Cn2c(-c3ccccc3)nc(OC)c2C=O)cc1)(=O)=O)=O
• CAS Number: 304462-19-9
• Cell Research: COS cells and CHO cells are stably transfected with rat Mas cDNA driven by a cytomegalovirus promoter and selected by neomycin. 125I-Ang-(1-7) (0.5x10^-9 mol/L) is incubated in 24-well plates for 60 minutes at 4 degree C in 0.3mL of serum-free medium (DMEM) supplemented with 0.2% BSA, 0.005% bacitracin, 0.1 mol/L PMSF, and 0.5 mol/L orthophenanthroline with Mas-transfected COS cells in the presence or absence of AVE 0991 (AVE, 10-10 to -5 mol/L). After 2 ishes with ice-cold serum-free DMEM, cells are disrupted with 0.1% Triton X-100. Bound radioactivity is measured in a gamma counter. Binding of rhodamine-Ang-(1-7) in Mas-transfected CHO cells is performed under similar conditions using 2x10^-9 mol/L rhodamine-labeled-Ang-(1-7) in the presence or absence of AVE (10^-6 mol/L), CV11974 (10^-6 mol/L), or PD123319 (10^-6 mol/L). NSB is determined in the presence of 10-6 mol/L Ang-(1-7) [1].
• Kinase Assay: Briefly, 100 ug of membranes from primary cultured bovine aortic endothelial cells (BAECs, passage 1) are incubated in a total volume of 200uL for 45 minutes at 25 degree C in HEPES-buffered saline (10mM HEPES, 0.1 M NaCl, 5mM MgCl2) containing 0.2% BSA and protease inhibitor cocktail Complete. Saturable binding of [125I]-Ang-(1-7) is calculated by subtracting nonspecific binding (40% to 50%), determined in the presence of 10uM unlabeled Ang-(1-7) from total binding. Competition experiments with increasing concentrations of AVE 0991 and unlabeled Ang-(1-7) are performed in the presence of 10nM [125I]-Ang-(1-7). Assays are terminated by vacuum filtration (<=15mM Hg) over filters (0.65uM, Opak 96-well plates) presoaked with 1% BSA. The filters are washed 3 times with each 100uL of PBS (50mM, NaHPO4 and 0.15M NaCl, pH 7.2). Radioactivity on dried filters is quantified with a gamma counter [1].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for AVE0991, inhibitor

AVE 0991 is a small molecular and orally active agonist of angiotensin-(1-7) receptor (IC50: 21nM).

Product Categories/Family for AVE0991, inhibitor

Endocrinology/Hormones; RAAS

References

Wiemer G, et al. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1-7) on the endothelium. Hypertension. 2002 Dec;40(6):847-52.
Wiemer G, et al. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1-7) on the endothelium. Hypertension. 2002 Dec;40(6):847-52.
Pinheiro SV, et al. Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct;44(4):490-6.
Pinheiro SV, et al. Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct;44(4):490-6.
Ferreira AJ, et al. The nonpeptide angiotensin-(1-7) receptor Mas agonist AVE-0991 attenuates heart failure induced by myocardial infarction. Am J Physiol Heart Circ Physiol. 2007 Feb;292(2):H1113-9.
Ferreira AJ, et al. The nonpeptide angiotensin-(1-7) receptor Mas agonist AVE-0991 attenuates heart failure induced by myocardial infarction. Am J Physiol Heart Circ Physiol. 2007 Feb;292(2):H1113-9.