Identification | Back Directory | [Name]
Odevixibat) | [CAS]
501692-44-0 | [Synonyms]
Odevixibat) A4250
(A-4250 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)- | [Molecular Formula]
C37H48N4O8S2 | [MDL Number]
MFCD32710220 | [MOL File]
501692-44-0.mol | [Molecular Weight]
740.93 |
Chemical Properties | Back Directory | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C, stored under nitrogen | [solubility ]
DMSO : 166.67 mg/mL (224.95 mM; Need ultrasonic) | [form ]
A solid | [pka]
3.32±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
Odevixib at is an orally activepotent and selective ileal bile acid transporter (IBAT; ASBT; SLC10A2) inhibitor th at improves cholestatic liver and bile duct injury in a mouse model of sclerosing cholangitis (0.01% w/w in diet). | [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. DOI:10.1016/j.jhep.2015.10.024 |
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Suzhou MgPlus Pharmtech Co., Ltd. Gold
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