N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide
AVE 0991
CAS: 304462-19-9
Molecular Formula: C29H32N4O5S2
N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide - Names and Identifiers
N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide - Physico-chemical Properties
| Molecular Formula | C29H32N4O5S2 |
| Molar Mass | 580.72 |
| Density | 1.31±0.1 g/cm3(Predicted) |
| Melting Point | 191-192℃ |
| Solubility | DMSO |
| pKa | 5.12±0.10(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | 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). |
| In vivo study | 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. |
N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.722 ml | 8.61 ml | 17.22 ml |
| 5 mM | 0.344 ml | 1.722 ml | 3.444 ml |
| 10 mM | 0.172 ml | 0.861 ml | 1.722 ml |
| 5 mM | 0.034 ml | 0.172 ml | 0.344 ml |
Last Update：2024-01-02 23:10:35
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Product Name: AVE 0991 Visit Supplier Webpage Request for quotation
CAS: 304462-19-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 304462-19-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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