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Eprosartan Mesylate

Name: Eprosartan Mesylate
Brand: Selleck Chemicals
SKU: S4102
Rating: 5 (4 reviews)

Synonyms: SKF-108566J

Catalog No.S4102 Purity: 99.99%

Eprosartan(SKF-108566J) is a nonpeptide angiotensin II receptor antagonist, [³H]-eprosartan binds to the AT1 receptor with K_D of 0.83 nM in rat vascular smooth muscle cells.

Eprosartan Mesylate Chemical Structure

CAS: 144143-96-4

Selleck's Eprosartan Mesylate has been cited by 4 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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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 K_D 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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