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25mg |
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100mg |
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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) with potential anti-inflammatory, immunomodulating and anti-viral activities. In inhibits DHODH with an IC50 of 134 nM for human DHODH.
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].
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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].
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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. |
Molecular Formula |
C20H18FNO4
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Molecular Weight |
355.36
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CAS # |
717824-30-1
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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
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.