Saralasin acetate hydrate
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate 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 acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension.
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- CAS No.: 39698-78-7
- Formule: C44H71N13O13
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
Ki: 0.32 nM (Angiotensin II receptor)[3]
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 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].
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.
In Vivo
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].
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.
Chemical Information
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CAS No. 39698-78-7
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Formule C44H71N13O13
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Synonyms
[Sar1,Ala8] Angiotensin II acetate hydrate
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Sequence Shortening
{Sar}-RVYVHPA
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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. 6/ [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Saralasin acetate hydrate Related Classifications
HY-P0205A Related Classifications
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