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编 号：F740660
分子式：C44H71N13O13
分子式：C44H71N13O13
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CAS No: 39698-78-7
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生物活性：
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
体内研究：
Saralasin acetate hydrate (intravenous injection, 5-50μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis.Saralasin acetate hydrate (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.Animal Model:Cerulein-induced acute pancreatitis rats model
Dosage:5, 10, 20, and 50 μg/kg, a single dose.
Administration:Intravenous injection
Result:Restored the pancreatic morphological characteristics to the control level.Reduced pancreatic injury and suppressed the glutathione depletion induced by cerulean.
Animal Model:Male Sprague-Dawley rats
Dosage:10 and 30 mg/kg, a single dose.
Administration:Subcutaneous injection
Result:Stimulated renin release without altering blood pressure or heart rate at the time of measuring serum renin levels 20 minutes after injection.
体外研究：
Saralasin acetate hydrate (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells.Saralasin acetate hydrate (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 acetate hydrate (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 acetate hydrate (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels.
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
体内研究：
Saralasin acetate hydrate (intravenous injection, 5-50μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis.Saralasin acetate hydrate (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.Animal Model:Cerulein-induced acute pancreatitis rats model
Dosage:5, 10, 20, and 50 μg/kg, a single dose.
Administration:Intravenous injection
Result:Restored the pancreatic morphological characteristics to the control level.Reduced pancreatic injury and suppressed the glutathione depletion induced by cerulean.
Animal Model:Male Sprague-Dawley rats
Dosage:10 and 30 mg/kg, a single dose.
Administration:Subcutaneous injection
Result:Stimulated renin release without altering blood pressure or heart rate at the time of measuring serum renin levels 20 minutes after injection.
体外研究：
Saralasin acetate hydrate (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells.Saralasin acetate hydrate (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 acetate hydrate (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 acetate hydrate (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels.
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