AVE 0991
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- CAS号:
- 304462-19-9
- 英文名:
- AVE0991
- 英文别名:
- AVE0991;N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide;N-[(Ethylamino)carbonyl]-3-[4-[(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)-2-thiophenesulfonamide;2-Thiophenesulfonamide, N-[(ethylamino)carbonyl]-3-[4-[(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)-
- 中文名:
- AVE 0991
- 中文别名:
- 化合物AVE 0991;ANG-(1-7)激动剂(AVE 0991);N-(乙基氨甲酰)-3-(4-((5-甲酰基-4-甲氧基-2-苯基-1H-咪唑-1-基)甲基)苯基)-5-异丁基噻吩-2-磺酰胺
- CBNumber:
- CB02669757
- 分子式:
- C29H32N4O5S2
- 分子量:
- 580.72
- MOL File:
- 304462-19-9.mol
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AVE 0991化学性质
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熔点:
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191-192℃
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密度:
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1.31±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2–8 °C
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溶解度:
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≥29.04 mg/mL in DMSO
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形态:
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solid
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酸度系数(pKa):
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5.12±0.10(Predicted)
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颜色:
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Off-white to yellow
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AVE 0991性质、用途与生产工艺
AVE 0991 是一种有效的非肽Ang-(1-7) 受体 Mas 激动剂。AVE 0991 与 [125I]-Ang-(1-7) 竞争性地结合到牛主动脉内皮细胞膜,IC50 为 21 nM。
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
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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
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: 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
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-15778 | AVE 0991 AVE 0991 | 304462-19-9 | 2mg | 950元 |
2024/04/30 | HY-15778 | AVE 0991 AVE 0991 | 304462-19-9 | 5mg | 1900元 |
304462-19-9, AVE 0991 相关搜索:
- 细胞生物学试剂
- C29H32N4O5S2
- 化合物AVE 0991
- N-(乙基氨甲酰)-3-(4-((5-甲酰基-4-甲氧基-2-苯基-1H-咪唑-1-基)甲基)苯基)-5-异丁基噻吩-2-磺酰胺
- ANG-(1-7)激动剂(AVE 0991)
- 304462-19-9
- N-(Ethylcarbamoyl)-3-(4-((5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl)phenyl)-5-isobutylthiophene-2-sulfonamide
- 2-Thiophenesulfonamide, N-[(ethylamino)carbonyl]-3-[4-[(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)-
- N-[(Ethylamino)carbonyl]-3-[4-[(5-formyl-4-methoxy-2-phenyl-1H-imidazol-1-yl)methyl]phenyl]-5-(2-methylpropyl)-2-thiophenesulfonamide
- AVE0991