Eprosartan Mesylate - CAS 144143-96-4
Catalog number: 144143-96-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H24N2O4S.CH4O3S
Molecular Weight:
520.62
COA:
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Targets:
Angiotensin Receptor
Description:
Eprosartan is a nonpeptide angiotensin II receptor antagonist, [3H]-eprosartan binds to the AT1 receptor with KD of 0.83 nM in rat vascular smooth muscle cells.
Purity:
>98%
MSDS:
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InChIKey:
DJSLTDBPKHORNY-XMMWENQYSA-N
InChI:
InChI=1S/C23H24N2O4S.CH4O3S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27;1-5(2,3)4/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29);1H3,(H,2,3,4)/b18-12+;
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
1.The angiotensin receptor blocker eprosartan mesylate reduces pulse pressure in isolated systolic hypertension.
Teitelbaum I1, Chilvers M, Reiz RJ. Can J Cardiol. 2004 Oct;20 Suppl C:11C-16C.
BACKGROUND: Isolated systolic hypertension (ISH) is a common and particularly poorly controlled form of hypertension.
2.Determination of eprosartan mesylate and hydrochlorothiazide in tablets by derivative spectrophotometric and high-performance liquid chromato
Hacioğlu F1, Onal A. J Chromatogr Sci. 2012 Sep;50(8):688-93. doi: 10.1093/chromsci/bms037. Epub 2012 May 10.
Two new simple and selective assay methods have been presented for the analysis of eprosartan mesylate (EPR) and hydrochlorothiazide (HCT) in pharmaceutical formulations. The first method is based on first-derivative ultraviolet spectrophotometry with zero-crossing measurements at 246 and 279 nm for EPR and HCT, respectively. The assay was linear over the concentration ranges 3.0-14.0 µg/mL for EPR and 1.0-12.0 µg/mL for HCT. The quantification limits for EPR and HCT were found to be 1.148 and 0.581 µg/mL, respectively, while the detection limits were 0.344 µg/mL for EPR and 0.175 µg/mL for HCT. The second method involved isocratic reversed-phase liquid chromatography using a mobile phase composed of acetonitrile-10 mM phosphoric acid (pH 2.5) (40:60, v/v). Olmesartan was used as internal standard and the substances were detected at 272 nm. The linearity ranges were found to be 0.5-30 and 0.3-15.0 µg/mL for EPR and HCT, respectively. The limits of detection were found to be 0.
3.Once-daily eprosartan mesylate in the treatment of elderly patients with isolated systolic hypertension: data from a 13-week double-blind, pl
Punzi HA1, Punzi CF. J Hum Hypertens. 2004 Sep;18(9):655-61.
This was a double-blind, randomized, placebo-controlled multicenter, titration-to-effect study of eprosartan in patients > or =60 years of age with isolated systolic hypertension. The study consisted of a 3 to 5-week placebo run-in period, a 13-week double-blind treatment period (6-week titration with eprosartan 600-1200 mg/day, 3-week maintenance, 4-week combination therapy with hydrochlorothiazide/HCTZ 12.5 mg), and a follow-up period within 5-7 days of last treatment dose. Overall, 283 patients (placebo/P: 135; eprosartan /E: 148) were randomized [female patients-P: 55.6%, E:54.7%; white-P:66.7%, E:67.6%). Mean sitting systolic blood pressure (SitSBP) at baseline was comparable (P: 170+/-0.8 mmHg; E: 171+/-0.8 mm Hg). At monotherapy end point, eprosartan produced a significant reduction in SitSBP (E: 16.1 mmHg vs P: 8.4 mmHg; P<0.0001). In all, 57.4% of patients responded to eprosartan monotherapy. Among nonresponders, the addition of HCTZ resulted in a decrease in SitSBP from baseline (E: 21.
4.Quality by design: a systematic and rapid liquid chromatography and mass spectrometry method for eprosartan mesylate and its related impuriti
Kalariya PD1, Kumar Talluri MV, Gaitonde VD, Devrukhakar PS, Srinivas R. J Sep Sci. 2014 Aug;37(16):2160-71. doi: 10.1002/jssc.201301364. Epub 2014 Jul 10.
The present work describes the systematic development of a robust, precise, and rapid reversed-phase liquid chromatography method for the simultaneous determination of eprosartan mesylate and its six impurities using quality-by-design principles. The method was developed in two phases, screening and optimization. During the screening phase, the most suitable stationary phase, organic modifier, and pH were identified. The optimization was performed for secondary influential parameters--column temperature, gradient time, and flow rate using eight experiments--to examine multifactorial effects of parameters on the critical resolution and generated design space representing the robust region. A verification experiment was performed within the working design space and the model was found to be accurate. This study also describes other operating features of the column packed with superficially porous particles that allow very fast separations at pressures available in most liquid chromatography instruments.
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CAS 144143-96-4 Eprosartan Mesylate

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