1. GPCR/G Protein
  2. Angiotensin Receptor
  3. AVE 0991

AVE 0991 

Cat. No.: HY-15778 Purity: 99.92%
Handling Instructions

AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.

For research use only. We do not sell to patients.

AVE 0991 Chemical Structure

AVE 0991 Chemical Structure

CAS No. : 304462-19-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 383 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of AVE 0991:

Top Publications Citing Use of Products

    AVE 0991 purchased from MCE. Usage Cited in: PLoS One. 2015 Nov 5;10(11):e0142087.

    The effect of AVE0991 on neuronal cell death following glucose deprivation. Data are shown for cells exposed to normal conditions (control) or glucose deprivation (vehicle) for 24 h or with (A) AVE0991 or (B) AVE0991+A779.

    AVE 0991 purchased from MCE. Usage Cited in: Redox Biol. 2019 Jan;20:75-86.

    AVE 0991 (AVE) treatment increases the expression of PKA-Cα, p-CREB, UCP-2, and Bcl-2, but the expression of Bax and Romo-1 are decreased in SAH+AVE group when compared with SAH+vehicle group.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.

    IC50 & Target

    IC50: 21±35 nM (Ang-(1-7) receptor)[1]

    In Vitro

    AVE 0991 is a nonpeptide compound that evokes effects similar to Ang-(1-7) on the endothelium. AVE 0991 and unlabeled Ang-(1-7) compete for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50s of 21±35 and 220±280 nM, respectively. Peak concentrations of NO and O2- release by AVE 0991 sodium salt and Ang-(1-7) (both 10 μM) are not significantly different (NO: 295±20 and 270±25 nM; O2-: 18±2 and 20±4 nM). However, the released amount of bioactive NO is ≈5 times higher for AVE 0991 in comparison to Ang-(1-7)[1].

    In Vivo

    AVE 0991 (0.58 nmol/g) produces a significant decrease of water diuresis in WT mice compared with vehicle-treated animals (0.06±0.03 mL versus 0.27±0.05; n=9 for each group; P<0.01). The antidiuretic effect of AVE 0991 (AVE) is associated with an increase in urine osmolality (1669±231.0 mOsm/KgH2O versus 681.1±165.8 mOsm/KgH2O in vehicle-treated mice; P<0.01). The genetic deletion of Mas abolishes the antidiuretic effect of AVE 0991 during water loading (0.37±0.10 mL [n=9] versus 0.27±0.03 mL [n=11] in AVE 0991-treated mice). As observed with C57BL/6 mice, administration of AVE 0991 (0.58 nmol/g) in water-loaded Swiss mice also produces a significant decrease of the urinary volume compared with vehicle-treated animals (0.13±0.05 mL [n=16] versus 0.51±0.04 mL [n=40]; P<0.01)[2]. One week of treatment with AVE-0991 produces a significant decrease in perfusion pressure (56.55±0.86 vs. 68.73±0.69 mmHg in vehicle-treated rats) and an increase in systolic tension (11.40±0.05 vs. 9.84±0.15 g in vehicle-treated rats), rate of tension rise (+dT/dt; 184.30±0.50 vs. 155.20±1.97 g/s in vehicle-treated rats), rate of tension fall (−dT/dt; 179.60±1.39 vs. 150.80±2.42 g/s in vehicle-treated rats). A slight increase in heart rate (HR) is also observed (220.40±0.71 vs. 214.20±0.74 beats/min in vehicle-treated rats[3].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (172.20 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7220 mL 8.6100 mL 17.2200 mL
    5 mM 0.3444 mL 1.7220 mL 3.4440 mL
    10 mM 0.1722 mL 0.8610 mL 1.7220 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.31 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    Binding of [125I]-Ang-(1-7) is performed. Briefly, 100 μg of membranes from primary cultured bovine aortic endothelial cells (BAECs, passage 1) are incubated in a total volume of 200 μL for 45 minutes at 25°C in HEPES-buffered saline (10 mM HEPES, 0.1 M NaCl, 5 mM MgCl2) containing 0.2% BSA and protease inhibitor cocktail Complete (Boehringer Mannheim). Saturable binding of [125I]-Ang-(1-7) is calculated by subtracting nonspecific binding (40% to 50%), determined in the presence of 10 μM 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 10 nM [125I]-Ang-(1-7). Assays are terminated by vacuum filtration (≤15 mm Hg) over Durapore filters (0.65 μm, Opak 96-well plates) presoaked with 1% BSA. The filters are washed 3 times with each 100 μL of PBS (50 mM, NaHPO4 and 0.15 M NaCl, pH 7.2). Radioactivity on dried filters is quantified with a gamma counter[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Monkey kidney (COS) cells and Chinese hamster ovary (CHO) cells are stably transfected with rat Mas cDNA driven by a cytomegalovirus promoter and selected by neomycin. 125I-Ang-(1-7) (0.5×10-9 mol/L) is incubated in 24-well plates for 60 minutes at 4°C in 0.3 mL 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 2×10-9 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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Mice[2]
    Swiss male mice, Mas-KO (Mas-/-) male mice on the pure genetic background C57BL/6, and WT C57BL/6 control mice (Mas+/+) are used. Water diuresis is induced by intraperitoneal water injection (0.05 mL/g of body weight [BW]) in conscious mice. Drugs are administered in the same injection with water load at prefixed volumes (0.01 mL/g BW). In the first set of experiments, WT mice (C57BL/6, control group) or Mas-KO mice are treated with: (1) 0.58 nmol/g AVE 0991 (n=9, control; n=11, Mas-KO mice); or (2) vehicle for AVE 0991 (10 μM KOH, 0.01 mL/g; n=9, control; n=9, Mas-KO). In the second set, Swiss mice are treated with: (1) vehicle (n=36); (2) 0.58 nmol/g AVE 0991 (n=16); (3) 46 pmol/g Ang-(1-7) antagonist A-779 (n=4); (4) 2 nmol/g losartan or valsartan (n=5); (5) 2 nmol/g AT2 receptor antagonists PD123319 or PD123177 (n=9); (6) AVE 0991 combined with A-779; (7) AVE 0991 combined with losartan or valsartan (n=4 for each); (8) or AVE 0991combined with PD123319 (n=5) or PD123177 (n=4). The urinary volume is measured for 60 minutes after water loading, and urine samples are obtained to determine the osmolality. The dose of AVE 0991is based in preliminary experiments performed in Swiss mice.
    Rats[3]
    Male Wistar rats weighting 250-300 g are used. Rats are treated either with AVE-0991 (1 mg/kg, n=9) or vehicle (0.9% NaCl, n=11) administered orally by gavage. At the end of the 7 day period of AVE-0991 treatment, the animals are decapitated 10-15 min after intraperitoneal injection of 400 IU of heparin. After the thorax is opened, the heart is carefully dissected, removed from the thoracic cavity, and placed in a plate containing ice-cold Krebs-Ringer solution (KRS) to attenuate any potential cardiac damage during dissection of aorta artery.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    580.72

    Formula

    C₂₉H₃₂N₄O₅S₂

    CAS No.

    304462-19-9

    SMILES

    O=S(C1=C(C2=CC=C(CN3C(C=O)=C(OC)N=C3C4=CC=CC=C4)C=C2)C=C(CC(C)C)S1)(NC(NCC)=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.92%

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    Product Name:
    AVE 0991
    Cat. No.:
    HY-15778
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    AVE 0991

    Cat. No.: HY-15778