产品
编 号：F436005
分子式：C20H18FNO4
分子量：355.36
分子式：C20H18FNO4
分子量：355.36
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 717824-30-1
产品详情
生物活性：
Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.
体内研究：
Vidofludimus (i.p.; once daily; for 14 days) exerts effects on dextran sodium sulfate (DSS) induced colitis in an FXR-dependent manner in vivo.Vidofludimus (p.o; 60 mg/kg; for 6 days) effectively improves many parameters of TNBS-induced colitis in rats and has inhibitory effects on colonic STAT3 and IL-17.Animal Model:homozygous FXR deficient (FXR KO) mice(10-week-old, male)
Dosage:20 mg/kg
Administration:oral, 20 mg/kg/day
Result:Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.
Animal Model:NAFLD Model(10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
Dosage:10 mg/kg
Administration:intraperitoneally, once daily, for 14 days
Result:Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice.Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).
Animal Model:Wistar rats
Dosage:60 mg/kg
Administration:p.o., for 6 days
Result:Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo.Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.
体外研究：
Vidofludimus (0-1 μM) selectively activats FXR in a concentration dependent manner with an EC50 value of about 450 nM in inducing the recruitment of various coactivator LXXLL motifs.Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway.Vidofludimus has inhibitory activity for human DHODH with an IC50 value of 160 nM.Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro.Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation.Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo.
Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.
体内研究：
Vidofludimus (i.p.; once daily; for 14 days) exerts effects on dextran sodium sulfate (DSS) induced colitis in an FXR-dependent manner in vivo.Vidofludimus (p.o; 60 mg/kg; for 6 days) effectively improves many parameters of TNBS-induced colitis in rats and has inhibitory effects on colonic STAT3 and IL-17.Animal Model:homozygous FXR deficient (FXR KO) mice(10-week-old, male)
Dosage:20 mg/kg
Administration:oral, 20 mg/kg/day
Result:Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.
Animal Model:NAFLD Model(10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
Dosage:10 mg/kg
Administration:intraperitoneally, once daily, for 14 days
Result:Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice.Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).
Animal Model:Wistar rats
Dosage:60 mg/kg
Administration:p.o., for 6 days
Result:Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo.Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.
体外研究：
Vidofludimus (0-1 μM) selectively activats FXR in a concentration dependent manner with an EC50 value of about 450 nM in inducing the recruitment of various coactivator LXXLL motifs.Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway.Vidofludimus has inhibitory activity for human DHODH with an IC50 value of 160 nM.Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro.Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation.Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备