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Vidofludimus
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vidofludimus图片
CAS NO:717824-30-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
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.
实验参考方法
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.