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AVE 0991

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Chemical Structure| 304462-19-9 同义名 : -
CAS号 : 304462-19-9
货号 : A125621
分子式 : C29H32N4O5S2
纯度 : 98%
分子量 : 580.718
MDL号 : MFCD27992063
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(68.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Angiotensin-(1–7) (Ang-[1–7]), a biologically active component of the renin-angiotensin system, regulates blood pressure by counteracting the vasoconstrictor and proliferative effects of Ang II. AVE 0991 is a novel nonpeptide compound that evoked effects similar to Ang-(1–7) on the endothelium. AVE 0991 competed for high-affinity binding of [125I]-Ang-(1–7) to bovine aortic endothelial cell membranes with IC50 values of 21 ± 35 nM (n=3). The released amount of bioactive NO was ≈5 times higher for AVE 0991 (10 μmol/L) in comparison to Ang-(1–7) (10 μmol/L)[3]. In water-loaded C57BL/6 mice, AVE 0991 (0.58 nmol/g body weight) produced a significant reduction in urinary volume (0.06+/-0.03 mL/60 min [n=9] versus 0.27+/-0.05 [n=9]; P<0.01), associated with an increase in urinary osmolality[4]. In infarcted male Wistar rats, AVE-0991 significantly attenuated the decrease in systolic tension (sham operated, 13.00 ± 1.02 g; infarction, 7.18 ± 0.66 g; AVE treated, 9.23 ± 1.05 g, n = 5), +dT/dt, -dT/dt, and heart rate induced by myocardial infarction. Furthermore, AVE-0991 significantly decreased the infarcted area (6.98 ± 1.01 vs. 3.94 ± 1.04 mm2 in AVE-treated rats)[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.61mL

1.72mL

0.86mL

17.22mL

3.44mL

1.72mL
参考文献

[1]Ferreira AJ, Jacoby BA, 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.

[2]Wiemer G, Dobrucki LW, et al. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1-7) on the endothelium. Hypertension. 2002 Dec;40(6):847-52.

[3]Wiemer G, Dobrucki LW, Louka FR, Malinski T, Heitsch H. AVE 0991, a nonpeptide mimic of the effects of angiotensin-(1-7) on the endothelium. Hypertension. 2002 Dec;40(6):847-52. doi: 10.1161/01.hyp.0000037979.53963.8f. PMID: 12468568.

[4]Pinheiro SV, Simões e Silva AC, Sampaio WO, de Paula RD, Mendes EP, Bontempo ED, Pesquero JB, Walther T, Alenina N, Bader M, Bleich M, Santos RA. Nonpeptide AVE 0991 is an angiotensin-(1-7) receptor Mas agonist in the mouse kidney. Hypertension. 2004 Oct;44(4):490-6. doi: 10.1161/01.HYP.0000141438.64887.42. Epub 2004 Aug 23. PMID: 15326087.

[5]Ferreira AJ, Jacoby BA, Araújo CA, Macedo FA, Silva GA, Almeida AP, Caliari MV, Santos RA. 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. doi: 10.1152/ajpheart.00828.2006. Epub 2006 Oct 20. PMID: 17056670.