1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Eprosartan

Eprosartan (Synonyms: SKF-108566J free base)

Cat. No.: HY-117743
Handling Instructions

Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .

For research use only. We do not sell to patients.

Eprosartan Chemical Structure

Eprosartan Chemical Structure

CAS No. : 133040-01-4

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Description

Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].

In Vitro

Eprosartan (SKF-108566J) inhibits [125I]AII binding to human liver membranes (IC50 of 1.7 nM) and to rat mesenteric artery membranes (IC50 of 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca2+ levels[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In conscious normotensive rats, i.v. administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

424.51

Formula

C₂₃H₂₄N₂O₄S

CAS No.
SMILES

O=C(C1=CC=C(C=C1)CN2C(/C=C(CC3=CC=CS3)/C(O)=O)=CN=C2CCCC)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (294.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3557 mL 11.7783 mL 23.5566 mL
5 mM 0.4711 mL 2.3557 mL 4.7113 mL
10 mM 0.2356 mL 1.1778 mL 2.3557 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EprosartanSKF-108566JAngiotensin Receptorangiotensin-IIantihypertensiveAT1nonpeptidInhibitorinhibitorinhibit

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Eprosartan
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