Bioactivity | 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[1][2][3]. | ||||||||||||
Invitro | 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[1].Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway[1].Vidofludimus has inhibitory activity for human DHODH with an IC50 value of 160 nM[2].Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro[3]. Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation[3].Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo[3]. Western Blot Analysis[1] Cell Line: | ||||||||||||
In Vivo | Vidofludimus (i.p.; once daily; for 14 days) exerts effects on dextran sodium sulfate (DSS) induced colitis in an FXR-dependent manner in vivo[1].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[3]. Animal Model: | ||||||||||||
Name | Vidofludimus | ||||||||||||
CAS | 717824-30-1 | ||||||||||||
Formula | C20H18FNO4 | ||||||||||||
Molar Mass | 355.36 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [1]. Yanlin Zhu, et al. Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD. Front Pharmacol. 2020 May 14;11:590. [2]. Andreas Muehler, et al. Vidofludimus calcium, a next generation DHODH inhibitor for the Treatment of relapsing-remitting multiple sclerosis. Mult Scler Relat Disord. 2020 Aug;43:102129. [3]. Leo R Fitzpatrick, et al. Vidofludimus inhibits colonic interleukin-17 and improves hapten-induced colitis in rats by a unique dual mode of action. J Pharmacol Exp Ther. 2012 Sep;342(3):850-60. |