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Eprosartan Mesylate (Synonyms: SKF 108566J)

Catalog No.GC16297

Angiotensin AT1 receptor antagonists

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Eprosartan Mesylate Chemical Structure

Cas No.: 144143-96-4

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10mM (in 1mL DMSO)
$37.00
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50mg
$47.00
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Sample solution is provided at 25 µL, 10mM.

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Background

Eprosartan mesylate (SKF-108566J) is a nonpeptide angiotensin II receptor antagonist with IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively. IC50 Value: 9.2 nM(in rat adrenal cortical membranes); 3.9 nM(in human adrenal cortical membranes)Target: Angiotensin Receptor Type-1(AT1)in vitro: Eprosartan mesylate, is one of the highly selective, orally active, non-peptide angiotensin-II-receptor antagonists [1]. In rat and human adrenal cortical membranes, Eprosartan displaced specifically bound [125I]AII with IC50 of 9.2 and 3.9 nM, respectively. Eprosartan also inhibited [125I]AII binding to human liver membranes (IC50 = 1.7 nM) and to rat mesenteric artery membranes (IC50 = 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca++ levels. In rabbit aortic rings [2].in vivo: Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr. In this same rat model, Eprosartan had no effect on base-line pressure or on the pressor response to norepinephrine or vasopressin [2]. Eprosartan is highly effective and safe in lowering blood pressure, notably SBP, in older subjects with mild to moderate hypertension [3]. Treatment with eprosartan in once-daily doses up to 1200 mg alone or in combination with HCTZ was well tolerated, with dizziness and asthenia being the most common side effects [4]. Therapy with eprosartan mesilat was associated with significant hypotensive effect (more evident in patients with high systolic blood pressure), improvement in 24-hour blood pressure profile and quality of life, and lower probability of secondary stroke. Side effects were not observed [5].

References:
[1]. Qian, J.J., et al., Eprosartan mesylate, an angiotensin II receptor antagonist. Acta Crystallogr Sect E Struct Rep Online, 2011. 67(Pt 4): p. o770-1.
[2]. Edwards, R.M., et al., Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther, 1992. 260(1): p. 175-81.
[3]. Conter, H.S., D.W. McKay, and R.J. Reiz, Eprosartan mesylate effectively reduces systolic and diastolic blood pressure in a Canadian primary care setting. Can J Cardiol, 2004. 20 Suppl C: p. 6C-10C.
[4]. Punzi, H.A. and C.F. Punzi, Once-daily eprosartan mesylate in the treatment of elderly patients with isolated systolic hypertension: data from a 13-week double-blind, placebo-controlled, parallel, multicenter study. J Hum Hypertens, 2004. 18(9): p. 655-61.
[5]. Martynov, M., et al., [Eprosartan mesylate in controlling of blood pressure in patients with ischemic stroke]. Zh Nevrol Psikhiatr Im S S Korsakova, 2002. 102(4): p. 26-30.

Chemical Properties

Cas No. 144143-96-4 SDF
Synonyms SKF 108566J
Chemical Name 4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid;methanesulfonic acid
Canonical SMILES CCCCC1=NC=C(N1CC2=CC=C(C=C2)C(=O)O)C=C(CC3=CC=CS3)C(=O)O.CS(=O)(=O)O
Formula C24H28N2O7S2 M.Wt 520.62
Solubility ≥ 22.15mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9208 mL 9.6039 mL 19.2079 mL
5 mM 0.3842 mL 1.9208 mL 3.8416 mL
10 mM 0.1921 mL 0.9604 mL 1.9208 mL
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