Home GPCR & G Protein Angiotensin Receptor antagonist Eprosartan Mesylate For research use only.

Eprosartan Mesylate

Synonyms: SKF-108566J

Eprosartan(SKF-108566J) 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.

Eprosartan Mesylate Chemical Structure

Eprosartan Mesylate Chemical Structure

CAS No. 144143-96-4

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Biological Activity

Description Eprosartan(SKF-108566J) 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.
Features At least 1,000- to 10,000-fold more selective for the AT1 than the AT2 receptor.
Targets
AT1 receptor [1]
0.83 nM(Kd)
In vitro
In vitro

Eprosartan inhibits [125I]-angiotensin II binding with IC50 1.4 nM to 3.9 nM in human tissues (adrenal cortex, liver, cloned AT1 receptor) and 1.5 nM to 9.2 nM in rat tissues (e.g. mesenteric artery, adrenal cortex, renal glomerulus). Eprosartan (100 nM), but not an AT2 antagonist, completely blocks angiotensin II-induced isotonic fluid absorption in rabbit isolated perfused proximal convoluted tubules. [1]
In Vivo
In vivo

Eprosartan (3 mg/kg-10 mg/kg, administered by duodenal or gastric catheter) also produces a dose-dependent inhibition of the pressor response to angiotensin II in conscious normotensive rats. Eprosartan (10 mg/kg) dose-dependently reduces blood pressure and antihypertensive activity is maintained for 1.5 hours in renin-dependent hypertensive rats. Eprosartan (60 mg/kg/day, intraperitoneally) is associated with no mortality (0 of 20 rats) after 18 weeks compared with a 100% mortality rate by week 9 among 20 vehicle-treated rats. Eprosartan (10 mg/kg) dose-dependently reduces mean arterial pressure and does not cause reflex tachycardia in dogs. Eprosartan (0.3 mg/kg) inhibits the pressor response induced by electronic stimulation of the spinal cord in the pithed rat. Eprosartan inhibits amino acid-induced glomerular hyperfiltration in rats. [1] Eprosartan (0.3 mg/kg i.v.) inhibits the pressor response induced by spinal cord stimulation in a manner similar to that observed with the peptide antagonist, Sar1, Ile8[angiotensin II] in the pithed rat. Eprosartan is more effective in inhibiting sympathetic nervous system activity compared to other chemically distinct nonpeptide angiotensin II receptor antagonists. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01562613 Completed
Hypertension|Stroke
Abbott
 March 2012 --
NCT04954560 Completed
Uric Acid Concentration Serum Quantitative Trait Locus 7
Medical University of Lodz
 January 1 2008 Not Applicable

Chemical Information & Solubility

Molecular Weight 520.62 Formula

C23H24N2O4S.CH4O3S
CAS No. 144143-96-4 SDF Download Eprosartan Mesylate SDF
Smiles CCCCC1=NC=C(N1CC2=CC=C(C=C2)C(=O)O)C=C(CC3=CC=CS3)C(=O)O.CS(=O)(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (192.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble


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In vivo
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