Eprosartan Mesylate

Catalog No.S4102

Eprosartan Mesylate Chemical Structure

Molecular Weight(MW): 520.62

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.

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  • (B) Dose-response curves of each drug for acute G protein or barr activation derived from the CellKey assay. LOS: Losartan; EXP: EXP3174; TEL: Telmisartan; EPR: Eprosartan; AZI: Azilsartan; OLM: Olmesartan; CAN: Candesartan; VAL: Valsartan; IRB: Irbesartan.

    Sci Rep, 2015, 5:8116.. Eprosartan Mesylate purchased from Selleck.

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Biological Activity

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.
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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 104 mg/mL (199.76 mM)
Ethanol 4 mg/mL (7.68 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 520.62
Formula

C23H24N2O4S.CH4O3S

CAS No. 144143-96-4
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID