Odevixibat-d₅  (Synonyms: A4250-d₅)

Odevixibat-d₅ is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis^[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.

Odevixibat (A4250)(0.01% (w/w) in chow diet; 4 weeks) improves sclerosing cholangitis and significantly reduces serum alanine aminotransferase, alkaline phosphatase and BAs levels, hepatic expression of pro-inflammatory and pro-fibrogenic genes and bile duct proliferation in Mdr2^-/- mice^[2].
In addition, Odevixibat (A4250) significantly reduces bile flow and biliary BA output, which correlates with reduced bsep transcription, while Ntcp and Cyp7a1 are induced^[2].

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

745.96

C₃₇H₄₃D₅N₄O₈S₂

501692-44-0

[2H]C1=C(C([2H])=C(C([2H])=C1[2H])N2CC(CCCC)(NS(=O)(C3=CC(OCC(N[C@H](C4=CC=C(C=C4)O)C(N[C@H](C(O)=O)CC)=O)=O)=C(C=C32)SC)=O)CCCC)[2H]

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]. Baghdasaryan A, et al. Inhibition of intestinal bile acid absorption improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis.J Hepatol. 2016 Mar;64(3):674-81.  [Content Brief]