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NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC 50 of 182 nM.
In Vitro
NFAT Transcription Factor Regulator-1 (compound example 19) inhibits IL-2 synthesis with an IC 50 of 182 nM. NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC 50 s of 82 and 146 nM, respectively. NFAT Transcription Factor Regulator-1 is able to inhibit IL-4 and IL-5 production in human T-cell lines with similar potency to its effects on IL-2 release. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NFAT Transcription Factor Regulator-1 is found to have an inhibitory potency approximately 10-fold better than that of cyclosporine. Comparable inhibitory effects on T-cell IL-2 production are obtained with NFAT Transcription Factor Regulator-1 and cyclosporine at doses of 3.0 and 30 mg/kg, po, respectively. The efficacies achieved in monkeys in vivo for blocking T-cell cytokine production suggest that NFAT Transcription Factor Regulator-1 has potential similar to that of cyclosporine for use in transplantation . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:IL-2 182 nM (IC 50 )
| Isomeric SMILES | C1=CC(=CC=C1NC(=O)C2=C(C=NC=C2)F)N3C(=CC(=N3)C(F)(F)F)OC(F)F |
|---|---|
| PubChem CID | 9931706 |
| Molecular Weight | 416.28 |
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