501692-44-0

501692-44-0 structure

Name: A4250
Chemical Name: odevixibat
CAS Number: 501692-44-0
Molecular Formula: C₃₇H₄₈N₄O₈S₂
Molecular Weight: 740.929
Catalog: Research Areas Metabolic Disease
Create Date: 2020-01-11 18:12:49
Modify Date: 2024-01-04 17:40:18
A4250 (A-4250, Odevixibat) is a small molecule ileal bile acid transporter (IBAT) inhibitor for the treatment of cholestatic liver diseases including progressive familial intrahepatic cholestasis and NASH. Other Indication Phase 3 Clinical

Name	odevixibat
Synonyms	odevixibat Butanoic acid, 2-[[(2R)-2-[[2-[[3,3-dibutyl-2,3,4,5-tetrahydro-7-(methylthio)-1,1-dioxido-5-phenyl-1,2,5-benzothiadiazepin-8-yl]oxy]acetyl]amino]-2-(4-hydroxyphenyl)acetyl]amino]-, (2S)- (2S)-2-{[(2R)-2-[({[3,3-Dibutyl-7-(methylsulfanyl)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl]oxy}acetyl)amino]-2-(4-hydroxyphenyl)acetyl]amino}butanoic acid

Description	A4250 (A-4250, Odevixibat) is a small molecule ileal bile acid transporter (IBAT) inhibitor for the treatment of cholestatic liver diseases including progressive familial intrahepatic cholestasis and NASH. Other Indication Phase 3 Clinical
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Metabolic Disease
Target	IC50: IBAT[1]
In Vivo	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[1]. In addition, Odevixibat (A4250) significantly reduces bile flow and biliary BA output, which correlates with reduced bsep transcription, while Ntcp and Cyp7a1 are induced[1]. Animal Model: Eight week old Mdr2-/- (Abcb4-/-) mice (model of cholestatic liver injury and sclerosing cholangitis)[1] Dosage: 0.01% (w/w) in chow diet Administration: 4 weeks Result: Decreased cholestatic liver and bile duct injury in mice model.
References	[1]. 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.