Eprosartan-d₆  (Synonyms: SKF-108566J free base-d₆)

Eprosartan-d₆ is deuterated labeled Eprosartan (HY-117743). 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].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
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^[2].

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

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^[2].

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

430.55

C₂₃H₁₈D₆N₂O₄S

133040-01-4

O=C(C1=C([2H])C([2H])=C(C([2H])=C1[2H])C([2H])([2H])N2C(/C=C(C(O)=O)\CC3=CC=CS3)=CN=C2CCCC)O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. R M Edwards, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81.  [Content Brief]