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MCE 国际站:Saralasin TFA
产品活性:Saralasin ([Sar1,Ala8] Angiotensin II) TFA 是血管紧张素 II (angiotensin II) 的八肽类似物。Saralasin TFA 是一种竞争性的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂,Ki 值为 0.32 nM (74% 的结合位点),并具有部分激动剂活性。Saralasin TFA 可用于肾血管性高血压、肾素依赖性(血管紧张素原性)高血压的相关研究。
研究领域:GPCR/G Protein
作用靶点:Angiotensin Receptor
In Vitro: Saralasin TFA (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells.
Saralasin TFA (5 μM, 2h) restores Ito, fast (Fast-Inactivating Transient Outward K+ Current in Mouse Ventricle) and I K, slow (Slow-Inactivating Transient Outward K+ Current in Mouse Ventricl) to control levels in myocytes.
Saralasin TFA (0.1-10 nM, 40 min) inhibits binding of FITC-Ang II to rat liver membrane preparation (used as the source of angiotensin receptors) with a Ki value of 0.32 nM for 74% of the binding sites and 2.7 nM for the remaining binding sites.
Saralasin TFA (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels.
In Vivo: Saralasin TFA (intravenous injection, 5-50 μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis.
Saralasin TFA (subcutaneous injection, 10 and 30 mg/kg, a single dose) increases serum renin activity (SRA) in normal, conscious rats, without markedly altering blood pressure or heart rate.
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