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Metabolism AhR Leflunomide

Leflunomide

Catalog No. T1159   CAS 75706-12-6
Synonyms: RS-34821, SU101, HWA486

Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Leflunomide, CAS 75706-12-6
Pack Size Availability Price/USD Quantity
25 mg In stock 36.00
50 mg In stock 47.00
100 mg In stock 58.00
200 mg In stock 81.00
500 mg In stock 180.00
1 mL * 10 mM (in DMSO) In stock 68.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.
Targets&IC50 AhR,   DHODH,   Protein-tyrosine kinase 2,  
Kinase Assay DHODase activity is measured by the DCIP colorimetric assay. This is a coupled assay in which oxidation of DHO and subsequent reduction of ubiquinone are stoichiometrically equivalent to the reduction of DCIP. Reduction of DCIP is accompanied by a loss of absorbance at 610 nm (ε=21500 M/cm). The assay is performed in a 96-well microtiter plate at ambient temperature (ca. 25°C). Stock solutions of 10 mM leflunomide and A771726 are prepared in dimethyl sulfoxide (DMSO) and these are diluted with reaction buffer (100 mM Tris and 0.1 % Triton X-100, pH 8.0) to prepare working stocks of the inhibitors at varying concentrations. For each reaction, the well contained 10 nM DHODase, 68 μM DCIP, 0.16 mg/mL gelatin, the stated concentration of ubiquinone, 10 μL of an inhibitor working stock to give the stated final concentration, and reaction buffer. After a 5-min equilibration period, the reaction is initiated by addition of DHO to the stated final concentrations. The total volume of reaction mixture for each assay is 150 μL, and the final DMSO concentration is ≤ 0.01% (v/v). The reaction progress is followed by recording the loss of absorbance at 610 nm over a 10-min period (during which the velocity remained linear). Velocities are reported as the change in absorbance at 610 nm per minute, and each reported value is the average of three replicates. In experiments where the DHO or ubiquinone concentration is varied, the other substrate is held constant at 200 μM. To determine the inhibitor potency of leflunomide and A771726, the effects of varying concentrations of the two compounds on the initial velocity of the DHODase reaction is measured over a concentration range of 0.01−1.0 μM. In these experiments the DHO and ubiquinone concentrations are held constant at 200 and 100 μM, respectively.
Synonyms RS-34821 , SU101 , HWA486
Purity 100.00%
Molecular Weight 270.21
Formula C12H9F3N2O2
CAS No. 75706-12-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 27 mg/mL (100 mM)

Ethanol: 27 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Davis JP, et al. Biochemistry, 1996, 35(4), 1270-1273. 2. Xu X, et al. J Biol Chem. 1995, 270(21), 12398-12403. 3. Fox RI, et al. Clin Immunol, 1999, 93(3), 198-208. 4. Ferrini MG, et al. Urology. 2006 Aug;68(2):429-35.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Neuronal Signaling Compound Library FDA-approved Drug Library Immunology/Inflammation Compound Library Kinase Inhibitor Library Fluorochemical Library Anti-Metabolism Disease Compound Library Killers Collection

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