AVE 0991
AVE 0991 性质
| 熔点 | 191-192℃ |
|---|---|
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 溶解度 | DMSO 中≥29.04 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 5.12±0.10(Predicted) |
| 颜色 | 米白色至黄色 |
| InChIKey | QTOZBSNPDCWHPV-UHFFFAOYSA-N |
| SMILES | O=CC(N1CC2=CC=C(C=C2)C3=C(SC(CC(C)C)=C3)S(NC(NCC)=O)(=O)=O)=C(N=C1C4=CC=CC=C4)OC |
AVE 0991 用途与合成方法
IC50: 21±35 nM (Ang-(1-7) receptor)
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 [ 125 I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC 50 s of 21±35 and 220±280 nM, respectively. Peak concentrations of NO and O 2 - release by AVE 0991 sodium salt and Ang-(1-7) (both 10 μM) are not significantly different (NO: 295±20 and 270±25 nM; O 2 - : 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).
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/KgH 2 O versus 681.1±165.8 mOsm/KgH 2 O 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). 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.
AVE 0991 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-15778 | AVE 0991 | 304462-19-9 | 2mg | 950 |
| 2025-12-22 | HY-15778 | AVE 0991 | 304462-19-9 | 5mg | 1900 |