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39698-78-7
2024/12/17 17:00:48

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。

体外研究:

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 I K, 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 Ki value 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 ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels[4].

体内研究:

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].


单字母 H2N-Sar-RVYVHPA-OH

CAS No. : 39698-78-7
多字母 H2N-Sar-Arg-Val-Tyr-Val-His-Pro-Ala-OH
氨基酸个数 8
分子式 C42H65N13O10
平均分子量(MW) 912.05
精确分子量(Exact Mass)(MW) 911.5
等电点(PI) -
pH=7.0时的净电荷数 3.21
GRAVY 0
亲水残基比例 -
消光系数 1490
溶解建议 疏水

参考文献:

Pressure-overload-induced angiotensin-mediated early remodeling in mouse heart【 doi: 10.1371/journal.pone.0176713

上篇: sGnRH-A acetate
下篇: LPYFD-NH2
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