Saralasin
Based on 1 Customer Validation
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin 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 can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.46%
- CAS 番号: 34273-10-4
- 分子式: C42H65N13O10
- 分子量:912.05
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保管条件:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Angiotensin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
Ki: 0.32 nM (Angiotensin II receptor)[3]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4 x 10-10 M
Compound: Saralasin
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Displacement of [125I][Sar, Ile]-ATII from human recombinant AT1 receptor expressed in HEK293 cells
Displacement of [125I][Sar, Ile]-ATII from human recombinant AT1 receptor expressed in HEK293 cells
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[PMID: 26988801] |
| HEK293 | IC50 |
4 x 10-10 M
Compound: Saralasin
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Displacement of [125I][Sar1,Ile8]-AT2 from human recombinant AT1 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [125I][Sar1,Ile8]-AT2 from human recombinant AT1 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
Saralasin (1 nM, 48 or 72 h) inhibits cell growth in 3T3 and SV3T3 cells[1].
Saralasin (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 (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 (1 μM, perfused rat ovary in vitro) inhibits the ovulation rate versus control and reduces prostaglandin E2 and 6-keto-prostaglandin F1α levels[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:3T3 and SV3T3 cells
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Concentration:1 nM
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Incubation Time:48 h, 72 h
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Result:Inhibited cell growth in 3T3 and SV3T3 cells and caused an increase of cellular renin concentration.
Saralasin (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cerulein-induced acute pancreatitis rats model[5]
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Dosage:5, 10, 20, and 50 μg/kg, a single dose.
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Administration:Intravenous injection
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Result:Restored the pancreatic morphological characteristics to the control level.
Reduced pancreatic injury and suppressed the glutathione depletion induced by cerulean.
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Animal Model:Male Sprague-Dawley rats[6]
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Dosage:10 and 30 mg/kg, a single dose.
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Administration:Subcutaneous injection
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Result:Stimulated renin release without altering blood pressure or heart rate at the time of measuring serum renin levels 20 minutes after injection.
化学情報
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CAS 番号 34273-10-4
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性状 Solid
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分子量 912.05
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分子式 C42H65N13O10
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Color White to off-white
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別名
[Sar1,Ala8] Angiotensin II
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配列
{Sar}-Arg-Val-Tyr-Val-His-Pro-Ala
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シーケンスの短縮
{Sar}-RVYVHPA
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
溶剤 & 溶解度
DMSO : 50 mg/mL (54.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
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. [Content Brief]
[2]. Jeremy H Kim, et al. Pressure-overload-induced angiotensin-mediated early remodeling in mouse heart. PLoS One. 2017 May 2;12(5):e0176713. [Content Brief]
[3]. Maziar Mohammad Akhavan, et al. A non-radioactive method for angiotensin II receptor binding studies using the rat liver. J Pharmacol Toxicol Methods. 2006 May-Jun;53(3):206-14. [Content Brief]
[4]. M Mikuni, et al. Saralasin-induced inhibition of ovulation in the in vitro perfused rat ovary is not replicated by the angiotensin II type-2 receptor antagonist PD123319. Am J Obstet Gynecol. 1998 Jul;179(1):35-40. [Content Brief]
[5]. Siu Po Ip, et al. Saralasin, a nonspecific angiotensin II receptor antagonist, attenuates oxidative stress and tissue injury in cerulein-induced acute pancreatitis. Pancreas. 2003 Apr;26(3):224-9. [Content Brief]
[6]. Campbell WB, et al. Saralasin-induced renin release: its blockade by prostaglandin synthesis inhibitors in the conscious rat. Hypertension. 1979;1(6):637‐642. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0964 mL | 5.4822 mL | 10.9643 mL | 27.4108 mL |
| 5 mM | 0.2193 mL | 1.0964 mL | 2.1929 mL | 5.4822 mL | |
| 10 mM | 0.1096 mL | 0.5482 mL | 1.0964 mL | 2.7411 mL | |
| 15 mM | 0.0731 mL | 0.3655 mL | 0.7310 mL | 1.8274 mL | |
| 20 mM | 0.0548 mL | 0.2741 mL | 0.5482 mL | 1.3705 mL | |
| 25 mM | 0.0439 mL | 0.2193 mL | 0.4386 mL | 1.0964 mL | |
| 30 mM | 0.0365 mL | 0.1827 mL | 0.3655 mL | 0.9137 mL | |
| 40 mM | 0.0274 mL | 0.1371 mL | 0.2741 mL | 0.6853 mL | |
| 50 mM | 0.0219 mL | 0.1096 mL | 0.2193 mL | 0.5482 mL |
Saralasin 関連分類
HY-P0205 関連分類
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