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Volixibat

Names

[ CAS No. ]:
1025216-57-2

[ Name ]:
Volixibat

[Synonym ]:
X2JZ0451H8
volixibat
3-O-Benzyl-N-({3-[(3S,4R,5R)-3-butyl-7-(dimethylamino)-3-ethyl-4-hydroxy-1,1-dioxido-2,3,4,5-tetrahydro-1-benzothiepin-5-yl]phenyl}carbamoyl)-6-O-sulfo-β-D-glucopyranosylamine
UNII:X2JZ0451H8
β-D-Glucopyranosylamine, 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]amino]carbonyl]-3-O-(phenylmethyl)-, 6-(hydrogen su lfate)

Biological Activity

[Description]:

Volixibat (SHP626) is a highly selective, minimally absorbed, and competitive apical sodium-dependent bile acid transporter (ASBT) inhibitor. Volixibat has potential for treatment for non-alcoholic steatohepatitis (NASH)[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[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[1]. Animal Model: Male Ldlr-/-.Leiden mice (high-fat diet, HFD)[1] 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.

[References]

[1]. Salic K, et al. Apical sodium-dependent bile acid transporter inhibition with volixibat improves metabolicaspects and components of non-alcoholic steatohepatitis in Ldlr-/-.Leiden mice. PLoS One. 2019 Jun 24;14(6):e0218459.

[2]. Palmer M, et al. A randomised, double-blind, placebo-controlled phase 1 study of the safety, tolerability and pharmacodynamics of volixibat in overweight and obese but otherwise healthy adults: implications for treatment of non-alcoholic steatohepatitis. BMC Pharmacol Toxicol. 2018 Mar 16;19(1):10.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C38H51N3O12S2

[ Molecular Weight ]:
805.954

[ Exact Mass ]:
805.291443

[ LogP ]:
5.35

[ Index of Refraction ]:
1.651

Related Compounds

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