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(Sar1,Val5,Ala8)-Angiotensin II

Names

[ CAS No. ]:
34273-10-4

[ Name ]:
(Sar1,Val5,Ala8)-Angiotensin II

[Synonym ]:
Saralasin
1-(N-Methylglycine)-5-L-valine-8-L-alanineangiotensin II
Sar-Arg-Val-Tyr-Val-His-Pro-Ala
H-Sar-Arg-Val-Tyr-Val-His-Pro-Ala-OH
1-Sar-8-ala-angiotensin II
M.W. 912.05 C42H65N13O10
N-Methylglycyl-N-(diaminomethylene)-L-ornithyl-L-valyl-L-tyrosyl-L-valyl-L-histidyl-L-prolyl-L-alanine
Sar-L-Arg-L-Val-L-Tyr-L-Val-L-His-L-Pro-L-Ala-OH
L-Alanine, N-methylglycyl-N-(diaminomethylene)-L-ornithyl-L-valyl-L-tyrosyl-L-valyl-L-histidyl-L-prolyl-
N-[1-[N-[N-[N-[N-[N2-(N-methylglycyl)-L-arginyl]-L-valyl]-L-tyrosyl]-L-valyl]-L-histidyl]-L-prolyl]-L-alanine
Sar-RVYVHPA
SAR-ARG-VAL-TYR-VAL-HIS-PRO-ALA-OH
MFCD00133980
[Sar1,Val5, Ala8] Angiotensin II
SAR-ARG-VAL-TYR-VAL-HIS-PRO-ALA: SAR-RVYVHPA
(Sar1,Val5,Ala8)-Angiotensin II

Biological Activity

[Description]:

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[1][3][6].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Research Areas >> Inflammation/Immunology
Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

[Target]

Ki: 0.32 nM (Angiotensin II receptor)[3]


[In Vitro]

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]. 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.

[In Vivo]

Saralasin (intravenous injection, 5-50 μg/kg, a single dose) ameliorates the oxidative stress and tissue injury in cerulein-induced pancreatitis[5]. 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]. 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.

[References]

[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.

[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.

[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.

[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]. Campbell WB, et al. Saralasin-induced renin release: its blockade by prostaglandin synthesis inhibitors in the conscious rat. Hypertension. 1979;1(6):637‐642.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C42H65N13O10

[ Molecular Weight ]:
912.047

[ Exact Mass ]:
911.497742

[ PSA ]:
355.05000

[ LogP ]:
-0.27

[ Index of Refraction ]:
1.654

[ Storage condition ]:
−20°C

Safety Information

[ WGK Germany ]:
3

Related Compounds

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