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AVE 0991 sodium salt

AVE 0991 sodium salt

产品编号 T14354   CAS 306288-04-0

AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes, with IC50 of 21±35 nM. AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist.

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AVE 0991 sodium salt Chemical Structure
AVE 0991 sodium salt, CAS 306288-04-0
规格 价格/CNY 货期 数量
2 mg ¥ 1,140 5日内发货
5 mg ¥ 1,930 5日内发货
10 mg ¥ 2,930 5日内发货
1 mL * 10 mM (in DMSO) ¥ 2,560 5日内发货

AVE 0991 sodium salt 的其他形式现货产品:

AVE 0991
其他形式的 AVE 0991 sodium salt:
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产品目录号及名称: AVE 0991 sodium salt (T14354)
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参考文献
产品描述 AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes, with IC50 of 21±35 nM. AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist.
靶点活性 Ang (1-7) receptor:21±35 nM
体外活性 AVE 0991 is a nonpeptide compound that evokes effects similar to Ang-(1-7) on the endothelium. 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), but the released amount of bioactive NO is ≈5 times higher for AVE 0991 in comparison to Ang-(1-7)[1]. 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.
体内活性 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). 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). 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]. 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). 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].
分子量 603.71
分子式 C29H32N4NaO5S2
CAS No. 306288-04-0

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (91.26 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6564 mL 8.2821 mL 16.5642 mL 41.4106 mL
5 mM 0.3313 mL 1.6564 mL 3.3128 mL 8.2821 mL
10 mM 0.1656 mL 0.8282 mL 1.6564 mL 4.1411 mL
20 mM 0.0828 mL 0.4141 mL 0.8282 mL 2.0705 mL
50 mM 0.0331 mL 0.1656 mL 0.3313 mL 0.8282 mL

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TargetMol Library Books参考文献

1. 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. 2. 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. 3. 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.

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Keywords

AVE 0991 sodium salt 306288-04-0 Others AVE 0991 sodium Inhibitor inhibitor inhibit

 

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