1025216-57-2

Name	Spebrutinib
CAS	1025216-57-2
Molecular Formula	C38H51N3O12S2
MDL Number	MFCD30747885
Molecular Weight	805.96
MOL File	1025216-57-2.mol

Synonyms

LUM002 SHP626 Urea, 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]-

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Chemical Properties

density	1.43±0.1 g/cm3(Predicted)
pka	-3.54±0.18(Predicted)

Hazard Information

Uses

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].

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. DOI:10.1371/journal.pone.0218459
[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. DOI:10.1186/s40360-018-0200-y

Supplier

HANGZHOU CLAP TECHNOLOGY CO.,LTD

Telephone86-571-88216897,88216896 13588875226

Websitehttp://www.hzclap.com/en/

Shanghai Easy CDMO Co.,Ltd

TelephoneInfo@easycdmo.com 13564957716

Website

Shandong Dayou Pharmaceutical Research and Development Co., Ltd.

Telephonedayouchem@126.com 15165037910

Website

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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