Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AVE 0991, a nonpeptide analog of angiotensin-(1-7) [Ang-(1-7)], is an orally active Mas agonist with inhibitory effects on [125I]-Ang-(1-7) binding to bovine aortic endothelial cell membranes, and inhibits astrocyte-mediated neuroinflammation in Alzheimer's disease by enhancing autophagy.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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2 mg | 在庫あり | ¥ 19,000 | |||
5 mg | 在庫あり | ¥ 34,000 | |||
10 mg | 在庫あり | ¥ 55,000 | |||
25 mg | 在庫あり | ¥ 105,500 | |||
50 mg | 在庫あり | ¥ 165,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 43,500 |
説明 | AVE 0991, a nonpeptide analog of angiotensin-(1-7) [Ang-(1-7)], is an orally active Mas agonist with inhibitory effects on [125I]-Ang-(1-7) binding to bovine aortic endothelial cell membranes, and inhibits astrocyte-mediated neuroinflammation in Alzheimer's disease by enhancing autophagy. |
ターゲット&IC50 | Ang (1-7) receptor:21±35 nM |
In vitro | AVE 0991 is a nonpeptide compound that elicits effects on the endothelium similar to Angiotensin-(1-7) [Ang-(1-7)]. 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. The peak concentrations of NO and O2- release induced by AVE 0991 sodium salt and Ang-(1-7) (both at 10 μM) show no significant difference (NO: 295±20 and 270±25 nM; O2-: 18±2 and 20±4 nM). However, the amount of bioactive NO released is approximately 5 times higher for AVE 0991 compared to Ang-(1-7)[1]. |
In vivo | In wild-type (WT) mice, the administration of AVE 0991 at a dose of 0.58 nmol/g leads to a significant reduction in water diuresis compared to vehicle-treated mice (0.06±0.03 mL versus 0.27±0.05; n=9 for each group; P<0.01). This antidiuretic effect of AVE 0991 is accompanied by 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, a receptor associated with the effects of AVE 0991, eliminates the antidiuretic impact 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). Similar to observations in C57BL/6 mice, the administration of AVE 0991 (0.58 nmol/g) in water-loaded Swiss mice also results in a significant reduction in urinary volume compared to vehicle-treated animals (0.13±0.05 mL [n=16] versus 0.51±0.04 mL [n=40]; P<0.01).Furthermore, a one-week treatment with AVE-0991 induces a notable 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). Additionally, there is an elevation in the rate of tension rise (+dT/dt; 184.30±0.50 vs. 155.20±1.97 g/s in vehicle-treated rats) and the 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) [4]. |
分子量 | 580.72 |
分子式 | C29H32N4O5S2 |
CAS No. | 304462-19-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: <0.1 mg/mL (Insoluble)
DMSO: 30 mg/mL(51.66 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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AVE 0991 304462-19-9 Others AVE0991 AVE-0991 Inhibitor inhibitor inhibit