中文名 | A-779 |
英文名 | (D-ALA7)-ANGIOTENSIN I/II (1-7) |
别名 | 化合物A 779(3TFA) 化合物PF-06447475 (D-ALA7)-血管紧张素I 5-L-异亮氨酸-7-D-丙氨酸-1-7-血管紧张素 II |
英文别名 | A-779 DRVYIHA A 779(3TFA) ASP-ARG-VAL-TYR-ILE-HIS-D-ALA H-ASP-ARG-VAL-TYR-ILE-HIS-D-ALA-OH |
CAS | 159432-28-7 |
化学式 | C39H60N12O11 |
分子量 | 872.97 |
密度 | 1.45±0.1 g/cm3(Predicted) |
酸度系数 | 3.29±0.10(Predicted) |
存储条件 | -15°C |
外观 | 冻干粉 |
颜色 | white to off-white |
体外研究 | A-779 inhibits the effect of Ang-(1-7), which suppresses the proliferating cell nuclear antigen (PCNA) protein expression up-regulated by Ang II, but A-779 alone has no effect to induce proliferation and migration of VSMCs. Pretreatment with Ang-(1-7) significantly retards Ang II-induced inflammatory responses of VSMCs associated with up-regulated MCP-1, VCAM-1 and IL-1β expressions, and this effect of Ang-(1-7) is blocked by A-779. But A-779 alone has no effect to induce inflammatory response of VSMCs. Pretreatment VSMCs with Ang-(1-7) for 5 min significantly inhibits Akt and ERK1/2 phosphorylation induced by Ang II, and this effect is also blocked by A-779, but alone has no effect to induce phosphorylation of Akt and ERK1/2 in VSMCs. |
体内研究 | Infusion of Ang(1-7) and A-779 (400 ng/kg/min, s.c.) alone or combined for 6 weeks does not prevent uterus atrophy or inhibit the body weight gain of OVX rats. A-779 markedly elevates serum bone specific alkaline phosphatase (BALP), telopeptides of collagen type I (CTX), tartarate resistant acid phosphatase (TRAcP 5b), osteocalcin (OC) and urinary deoxypyridinoline (DPD). Infusion of Ang(1-7) and/or A-779 does not significantly change serum minerals concentrations in sham or OVX groups. A-779 in the OVX animals does not change AngII, Ang(1-7), AT1R, AT2R, ACE, ACE-2, Mas receptor, RANKL and OPG proteins expressions in relation to OVX group, while AngII (P [1] . Inhibition of Ang1-7 cascade by A-779 (400 ng/kg/min) significantly eradicates captopril protective effects on bone metabolism, mineralization and micro-structure. A-779 also restores OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulates OPG expression and ACE-2/Ang1-7/Mas pathway. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.146 ml | 5.728 ml | 11.455 ml |
5 mM | 0.229 ml | 1.146 ml | 2.291 ml |
10 mM | 0.115 ml | 0.573 ml | 1.146 ml |
5 mM | 0.023 ml | 0.115 ml | 0.229 ml |
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