Volixibat

CAS No. 1025216-57-2

Volixibat( SHP-626 | SAR-548304 | LUM-002 )

Catalog No. M10116 CAS No. 1025216-57-2

A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Volixibat
  • Note
    Research use only, not for human use.
  • Brief Description
    A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH).
  • Description
    A highly potent and selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT) in development for the treatment of nonalcoholic steatohepatitis (NASH).Steatohepatitis Phase 2 Clinical.
  • In Vitro
    ——
  • In Vivo
    Volixibat (SHP626) (5-30 mg/kg; food intake; daily for 24 weeks) improves metabolic aspects and components of non-alcoholic steatohepatitis in Ldlr-/-.Leiden mice. Animal Model:Male Ldlr-/-.Leiden mice (high-fat diet, HFD)Dosage:5, 15, or 30 mg/kg Administration:Food intake; daily for 24 weeks.Result:Significantly increased the total amount of bile acid in feces. Significantly attenuated the HFD-induced increase in hepatocyte hypertrophy, hepatic triglyceride and cholesteryl ester levels, and mesenteric white adipose tissue deposition at the highest dose. Non-alcoholic fatty liver disease activity score (NAS) was significantly lower in volixibat-treated mice than in the HFD controls.
  • Synonyms
    SHP-626 | SAR-548304 | LUM-002
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    ASBT Transporter
  • Recptor
    ASBT Transporter
  • Research Area
    Other Indications
  • Indication
    Steatohepatitis

Chemical Information

  • CAS Number
    1025216-57-2
  • Formula Weight
    805.96
  • Molecular Formula
    C38H51N3O12S2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C(NC1=CC=CC([C@H](C2=CC(N(C)C)=CC=C23)[C@@H](O)[C@](CC)(CCCC)CS3(=O)=O)=C1)N[C@H]4[C@@H]([C@H]([C@@H]([C@@H](COS(=O)(O)=O)O4)O)OCC5=CC=CC=C5)O
  • Chemical Name
    N-[3-[(3S,4R,5R)-3-Butyl-7-(dimethylamino)-3-ethyl-2,3,4,5-tetrahydro-4-hydroxy-1,1-dioxido-1-benzothiepin-5-yl]phenyl]-N'-[3-O-(phenylmethyl)-6-O-sulfo-β-D-glucopyranosyl]urea

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Siebers N, et al. Eur J Drug Metab Pharmacokinet. 2017 Jul 12. doi: 10.1007/s13318-017-0429-7. 2. Tiessen RG, et al. BMC Gastroenterol. 2018 Jan 5;18(1):3.
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