NFAT Transcription Factor Regulator-1

Research use only, not for human use.

NFAT Transcription Factor Regulator-1 is an synthesis inhibitor of IL-2 (IC50 of 182 nM).

NFAT Transcription Factor Regulator-1 is an synthesis inhibitor of IL-2 (IC50 of 182 nM).(In Vitro):NFAT Transcription Factor Regulator-1 inhibits IL-2 synthesis(IC50 of 182 nM). NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC50s 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.(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.

NFAT Transcription Factor Regulator-1 (compound example 19) inhibits IL-2 synthesis with an IC50 of 182 nM. NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC50s 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.

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.

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Apoptosis

IL Receptor

PEGs

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245747-71-1

416.283

C17H10F6N4O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (240.22 mM)

FC(F)Oc1cc(nn1-c1ccc(NC(=O)c2ccncc2F)cc1)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years