Eprosartan Mesylate

SKU: orb1305350

Description

Eprosartan Mesylate (SKF-108566J) is a selective, competitive antagonist of the angiotensin II type 1 (AT1) receptor. It is widely used in cardiovascular research to study hypertension mechanisms and has been utilized in both in vitro receptor binding assays and in vivo animal models of blood pressure regulation.

Research Area

Metabolism Research

Key Properties

• CAS Number: 144143-96-4
• MW: 520.62
• Purity: 100.00%
• Formula: C₂₃H₂₄N₂O₄S·CH₄O₃S
• SMILES: s1c(C/C(=C\c2n(c(nc2)CCCC)Cc2ccc(cc2)C(=O)O)/C(=O)O)ccc1.S(=O)(=O)(O)C
• Target: RAAS
• Solubility: Ethanol:4 mg/mL (7.68 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.68 mM);DMSO:104 mg/mL (199.76 mM)

Bioactivity

• Target IC50:
  AT1 receptor:0.83 nM(Kd)
• In Vivo:
  Eprosartan effectively inhibits [125I]-Angiotensin II in human tissues (adrenal cortex, liver, cloned AT1 receptors) with an IC50 range of 1.4-3.9 nM and in rat tissues (mesenteric artery, adrenal cortex, glomeruli) with an IC50 range of 1.5-9.2 nM. In isolated perfused proximal tubules of rabbits, Eprosartan (100 nM) completely blocks the isosmotic fluid absorption induced by Angiotensin II.
• In Vitro:
  In a study involving brain and spinal cord injured rats, Eprosartan (0.3 mg/kg i.v.) was observed to induce a hypertensive response following spinal cord stimulation.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Angiotensin Receptor, angiotensin-II, antihypertensive, AT1, AT1 receptor, Eprosartan, Eprosartan Mesylate, Inhibitor, inhibit, nonpeptid, SKF-108566J

Compound Identifiers

PubChem CID

5282474