Vidofludimus

Alias: 4SC101; SC-12267;SC12267, 4SC-101;4SC 101; SC 12267.
Cat No.:V0861 Purity: ≥98%
Vidofludimus (4SC101; SC-12267;SC12267, 4SC-101;4SC 101; SC 12267) is a novel, potent and orally bioactive/bioavailable inhibitor of dihydroorotate dehydrogenase (DHODH) withpotentialanti-inflammatory,immunomodulatingandanti-viralactivities.
Vidofludimus Chemical Structure CAS No.: 717824-30-1
Product category: Dehydrogenase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
25mg
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Other Sizes

Other Forms of Vidofludimus:

  • Vidofludimus hemicalcium (4sc-101 hemicalcium; SC12267 hemicalcium)
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Vidofludimus (0-1 µM) selectively activates FXR in a concentration-dependent manner, with an EC50 value of approximately 450 nM, inducing the recruitment of various coactivator LXXLL motifs [1]. Vidofludimus (0-8 µM) inhibits nuclear translocation of p65 by suppressing the IKK-IκB-NF-κB pathway [1]. Vidofludimus inhibits human DHODH with an IC50 of 160 nM [2]. Vidofludimus inhibits dihydroorotate dehydrogenase and lymphocyte proliferation in vitro[3]. Vidofludimus inhibits interleukin (IL)-17 secretion in vitro, regardless of the effects on lymphocyte proliferation [3]. Vidofludimus completely inhibits IL-23 + IL-1β-stimulated IL-17 secretion by colonic strips in ex vivo[3].
ln Vivo
In vivo, vidofludimus (ip; once daily; for 14 days) affects colitis produced by dextran sodium sulfate (DSS) in a way that is dependent on FXR[1]. Vidofludimus (po; 60 mg/kg; for 6 days) inhibits colonic STAT3 and IL-17 and successfully improves numerous parameters of TNBS-induced colitis in rats[3].
Cell Assay
Western Blot Analysis[1]
Cell Types: HepG2 cells or MEFs
Tested Concentrations: 2, 8 μM
Incubation Duration: 1 h
Experimental Results: Inhibited of TNFα-induced IKKα/β phosphorylation and IκBα degradation.

RT-PCR[1]
Cell Types: HepG2 cells
Tested Concentrations: 5 μM
Incubation Duration: 24 h
Experimental Results: Inhibited the increase of NF-κB target genes MCP-1 and CXCL-2 upon TNFα stimulation.
Animal Protocol
Animal/Disease Models: homozygous FXR deficient (FXR KO) mice[1] (10weeks old, male)
Doses: 20 mg /kg
Route of Administration: po (oral gavage) 20 mg/kg/day
Experimental Results: Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.

Animal/Disease Models: NAFLD Model[1] (10-11 weeks old male obese Lepob/ob C57BL /6 (ob/ob) mice)
Doses: 10 mg/kg
Route of Administration: intraperitoneally, one time/day, for 14 days
Experimental Results: Dramatically decreased body weight loss, prevented colonic shortening, diminished histological scores, and disease activity index (DAI) scores in WT mice. Dramatically diminished colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).

Animal/Disease Models: Wistar rats[3]
Doses: 60 mg/kg
Route of Administration: po, for 6 days
Experimental Results: Effectively decreased macroscopic and histological pathology and the numbers of CD3+ T cells in vivo. decreased nuclear signal transducer and activator of transcription 3 (ST
References
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H18FNO4
Molecular Weight
355.36
CAS #
717824-30-1
SMILES
FC1C([H])=C(C2C([H])=C([H])C([H])=C(C=2[H])OC([H])([H])[H])C([H])=C([H])C=1N([H])C(C1=C(C(=O)O[H])C([H])([H])C([H])([H])C1([H])[H])=O
Synonyms
4SC101; SC-12267;SC12267, 4SC-101;4SC 101; SC 12267.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8140 mL 14.0702 mL 28.1405 mL
5 mM 0.5628 mL 2.8140 mL 5.6281 mL
10 mM 0.2814 mL 1.4070 mL 2.8140 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • 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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