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 competitiveangiotensin II receptorantagonist with aKivalue 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[1][3][6]. |
IC50& Target | Ki: 0.32 nM (Angiotensin II receptor)[3] |
体外研究 (In Vitro) | Saralasin TFA (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells[1]. Saralasin TFA (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 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 Kivalue of 0.32 nM for 74% of the binding sites and 2.7 nM for the remaining binding sites[3]. Saralasin TFA (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 TFA (intravenous injection, 5-50 μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis[5]. 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[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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分子量 | |
性状 | |
Formula | |
Sequence | {Sar}-Arg-Val-Tyr-Val-His-Pro-Ala |
Sequence Shortening | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | 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 1 mM | 0.9746 mL | 4.8730 mL | 9.7459 mL | 5 mM | 0.1949 mL | 0.9746 mL | 1.9492 mL | 10 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (97.46 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.44 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (2.44 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.44 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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