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    Vidofludimus
    Vidofludimus

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0861
    CAS #: 717824-30-1Purity ≥98%

    Description: Vidofludimus (4SC101;  SC-12267; SC12267, 4SC-101; 4SC 101; SC 12267) is a novel, potent and orally bioactive/bioavailable inhibitor of dihydroorotate dehydrogenase (DHODH) with potential anti-inflammatory, immunomodulating and anti-viral activities. In inhibits DHODH with an IC50 of 134 nM for human DHODH.

    References: Am J Pathol. 2010 Jun;176(6):2840-7; J Pharmacol Exp Ther. 2012 Sep;342(3):850-60. 

    Related CAS #: 1354023-23-6 (tris);717824-30-1 (free acid); 2245772-26-1 (sodium); 1354012-90-0 (Calium); 1354013-27-6 (potassium);  

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    Molecular Weight (MW)355.36
    FormulaC20H18FNO4
    CAS No.717824-30-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (281.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)

    Chemical Name: 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)carbamoyl)cyclopent-1-enecarboxylic acid

    InChi Key: XPRDUGXOWVXZLL-UHFFFAOYSA-N

    InChi Code: InChI=1S/C20H18FNO4/c1-26-14-5-2-4-12(10-14)13-8-9-18(17(21)11-13)22-19(23)15-6-3-7-16(15)20(24)25/h2,4-5,8-11H,3,6-7H2,1H3,(H,22,23)(H,24,25)

    SMILES Code: COC1=CC=CC(C2=CC(F)=C(NC(C3=C(C(O)=O)CCC3)=O)C=C2)=C1           

    Synonyms4SC101;  SC-12267; SC12267, 4SC-101; 4SC 101; SC 12267.


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    In Vitro

    In vitro activity: Vidofludimus causes a concentration dependent inhibition of phytohemagglutinin-stimulated PBMC proliferation via the inhibition of pyrimidine de novo synthesis. Vidofludimus attenuates IL-17 secretion from colonic strips by inhibition of STAT3 and NF-κB activation.


    Kinase Assay:  In vitro DHODH inhibition assay mixture contains 50 μM decycloubiquinone, 100 μM dihydroorotate, and 60 μM 2,6-dichloroindophenol. The amount of enzyme is adjusted such that an average slope of approximately 0.2 AU/min will be achieved in the assay for the positive control (eg, without inhibitor). Measurements are conducted in 50 mM TrisHCl, 150 mM KCl, 0.1% Triton X-100, and pH 8.0 at 30°C in a final volume of 1 ml. The components are mixed, and the reaction is started by adding dihydroorotate. The reaction is followed spectrophotometrically by measuring the decrease in absorption at 600 nm for 2 minutes. The assay is linear in time and enzyme concentration. Inhibitory studies are conducted in a standard assay with additional variable amounts of inhibitor. For the determination of the IC50 values (concentration of inhibitor required for 50% inhibition), eight different inhibitor concentrations are applied. Each data point is recorded in triplicates on a single measurement day. 


    Cell Assay:  Vidofludimus (4SC-101, SC12267) has been reported to dose-dependently inhibit DHODH in an in vitro enzyme assay with IC50 values of 0.134μmol/L, 1.29μmol/L, 10.6μmol/L and 12.9μmol/L in human DHODH, rat DHODH, mouse DHODH and human PBMC, respectively. In addition, Vidofludimus has shown the inhibition of proliferation in phytohemagglutinin-induced lymphocytes with an IC50 value of ~13μmol/L. Moreover, Vidofludimus has been revealed to concentration-dependently inhibit phytohemagglutinin-stimulated interukin-17 secretion from human peripgeral blppd mononuclear cell lines (PBMCs) with an IC50 value of 6 μmol/L.

    In VivoIn MRLlpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. In Rats, Vidofludimus (60 mg/kg, p.o.) effectively reduces macroscopic and histological pathology and the numbers of CD3+ T cells. In a rat model of renal transplantation, Vidofludimus (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection
    Animal modelMRLlpr/lpr mice 
    Formulation & DosageSuspended in water; 300 mg/kg; p.o. administration 
    References

    Am J Pathol. 2010 Jun;176(6):2840-7; J Pharmacol Exp Ther. 2012 Sep;342(3):850-60. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Vidofludimus

    Pharmacokinetics of 4SC-101 in mice.



    Vidofludimus
    4SC-101 reduces systemic autoimmunity in MRLlpr/lpr mice. Am J Pathol. 2010 Jun;176(6):2840-7. Am J Pathol. 2010 Jun;176(6):2840-7. 
     

    Vidofludimus

    4SC-101 and cutaneous lupus in MRLlpr/lpr mice. MRLlpr/lpr mice of all groups were regularly checked for skin manifestations, which typically occur in the facial or neck area. Am J Pathol. 2010 Jun;176(6):2840-7. Am J Pathol.2010 Jun;176(6):2840-7. 
     

    Vidofludimus

    4SC-101 improves GFR and proteinuria in MRLlpr/lpr mice.


    Vidofludimus

    4SC-101 improves renal histopathology in MRLlpr/lpr mice. Am J Pathol. 2010 Jun;176(6):2840-7. 


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