Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate 是血管紧张素 II (angiotensin II) 的八肽类似物。Saralasin acetate 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 acetate 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。
| 生物活性 | Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitiveangiotensin II receptorantagonist with aKivalue 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[1][3][6]. |
| IC50& Target | Ki: 0.32 nM (Angiotensin II receptor)[3] |
体外研究
(In Vitro) | Saralasin acetate hydrate (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells[1].
Saralasin acetate hydrate (5 μM, 2h) restores Ito, fast(Fast-Inactivating Transient Outward K+ Current in Mouse Ventricle) and IK, slow(Slow-Inactivating Transient Outward K+ Current in Mouse Ventricl) to control levels in myocytes[2].
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 Kivalue of 0.32 nM for 74% of the binding sites and 2.7 nM for the remaining binding sites[3].
Saralasin acetate hydrate (1 μM, perfused rat ovaryin vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1αlevels[4].
Cell Proliferation Assay[1] | Cell Line: | 3T3 and SV3T3 cells | | Concentration: | 1 nM | | Incubation Time: | 48 h, 72 h | | Result: | Inhibited cell growth in 3T3 and SV3T3 cells and caused an increase of cellular renin concentration. |
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体内研究
(In Vivo) | Saralasin acetate hydrate (intravenous injection, 5-50 μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis[5].
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[6].
| Animal Model: | Cerulein-induced acute pancreatitis rats model[5] | | 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[6] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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