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Eprosartan (mesylate) (CAS 144143-96-4) LS-H77

AT1 receptor antagonist
LS-H77-10 / 10 mg / $185
LS-H77-50 / 50 mg / $245
LS-H77-100 / 100 mg / $315
USA Shipment Only
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Description: Angiotensin II, as part of the renin-angiotensin-aldosterone system, facilitates a sympathetic nervous system response mediated by the angiotensin II type 1 (AT1) receptor, causing vasoconstriction and subsequent increase in blood pressure. It potentiates noradrenaline release from sympathetic nerve terminals at the presynaptic level as well as amplifies the alpha -adrenoceptor-mediated vasoconstrictor response to endogenous noradrenaline. Angiotensin II receptor blockers (ARBs) are a major class of therapeutics designed to lower blood pressure and to provide cardiovascular protection. Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 – 3.9 nM and an elimination half-life of five to seven hours. Eprosartan is structurally distinct from other noncompetitive ARBs in that it does not contain a biphenyl, tetrazole moiety and blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels. H77_ChemicalStructureImage.png
(αE)-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene]-2-thiophenepropanoic acid, mesylate
SKF108566J
biochemical, chemical, antagonist
LS-H77
144143-96-4
C23H24N2O4S • CH3SO3H
≥98%
A crystalline solid
 
CCCCC1=NC=C(/C=C(CC2=CC=CS2)/C(O)=O)N1CC3=CC=C(C(O)=O)C=C3.O=S(O)(C)=O
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+;
DJSLTDBPKHORNY-XMMWENQYSA-N
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: AGTR1 / AT1 Receptor related products

Usage Information

Eprosartan (mesylate) is supplied as a crystalline solid. A stock solution may be made by dissolving the eprosartan (mesylate) in the solvent of choice. Eprosartan (mesylate) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of eprosartan (mesylate) in ethanol is approximately 1 mg/ml and approximately 30 mg/ml in DMSO and DMF. Eprosartan (mesylate) is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, eprosartan (mesylate) should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Eprosartan (mesylate) has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Munger, M.A. Use of angiotensin receptor blockers in cardiovascular protection: Current evidence and future directions. PT 36(1), 22-40 (2011).
  2. Blankestijn, P.J. and Rupp, H. Clinical profile of eprosartan: A different angiotensin II receptor blocker. Cardiovasc. Hematol. Agents Med. Chem. 6(4), 253-257 (2008).
  3. Burnier, M. Angiotensin II type 1 receptor blockers. Circulation 103, 904-912 (2001).

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