Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
产品详情
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。
生物活性
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a K i value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
性状
Solid
IC50 & Target[1][2]
Ki: 0.32 nM (Angiotensin II receptor)
体外研究(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. has not independently confirmed the accuracy of these methods.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
SequenceShortening
{Sar}-RVYVHPA
Sequence
{Sar}-Arg-Val-Tyr-Val-His-Pro-Ala
参考文献
[1]. P Schelling, et al. Effects of angiotensin II and angiotensin II antagonist saralasin on cell growth and renin in 3T3 and SV3T3 cells. J Cell Physiol. 1979 Mar;98(3):503-13. [2]. Jeremy H Kim, et al. Pressure-overload-induced angiotensin-mediated early remodeling in mouse heart. PLoS One. 2017 May 2;12(5):e0176713.
溶解度数据
In Vitro: H2O : 100 mg/mL (97.46 mM; Need ultrasonic)DMSO : 50 mg/mL (48.73 mM; Need ultrasonic)配制储备液