Elobixibat-d₅  (Synonyms: A 3309-d₅; AZD 7806-d₅)

Elobixibat-d₅ is the deuterium labeled Elobixibat (HY-15790). Elobixibat (A 3309; AZD 7806) is orally active, bile acid transporter (IBAT) inhibitor with IC₅₀ values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to treat metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly^[1][2][3][4].

IC50: 0.53±0.17 nM (human IBAT), 0.13±0.03 nM (mouse IBAT), 5.8±1.6 nM (canine IBAT)^[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].

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

700.92

C₃₆H₄₀D₅N₃O₇S₂

439087-18-0

O=C(COC(C=C1C(N(CC(CCCC)(CCCC)CS1(=O)=O)C2=C([2H])C([2H])=C([2H])C([2H])=C2[2H])=C3)=C3SC)N[C@@H](C(NCC(O)=O)=O)C4=CC=CC=C4

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;53(2):211-216.  [Content Brief]

  [2]. Wong BS, et al. Elobixibat for the treatment of constipation. Expert Opin Investig Drugs. 2013 Feb; 22(2):277-84.  [Content Brief]

  [3]. Sugiyama Y, et al. Impact of elobixibat on liver tumors, microbiome, and bile acid levels in a mouse model of nonalcoholic steatohepatitis. Hepatol Int. 2023 Dec;17(6):1378-1392.  [Content Brief]

  [4]. Yamauchi R, et al. Elobixibat, an ileal bile acid transporter inhibitor, ameliorates non-alcoholic steatohepatitis in mice. Hepatol Int. 2021 Apr;15(2):392-404.  [Content Brief]