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ChemicalBook--->CAS DataBase List--->245747-71-1

245747-71-1

245747-71-1 Structure

245747-71-1 Structure
IdentificationBack Directory
[Name]

NFAT Transcription Factor Regulator
[CAS]

245747-71-1
[Synonyms]

NFAT Transcription Factor Regulator
NFAT Transcription Factor Regulator-1
4-Pyridinecarboxamide, N-[4-[5-(difluoromethoxy)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-
[Molecular Formula]

C17H10F6N4O2
[MDL Number]

MFCD31715449
[MOL File]

245747-71-1.mol
[Molecular Weight]

416.28
Chemical PropertiesBack Directory
[Boiling point ]

408.4±45.0 °C(Predicted)
[density ]

1.53±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 150 mg/mL (360.33 mM);Water : < 0.1 mg/mL (insoluble)
[form ]

Solid
[pka]

9.85±0.70(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Uses]

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
[Biological Activity]

NFAT Transcription Factor Regulator-1 is an inhibitor of IL-2 synthesis with IC50 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.

[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[1].

[target]

IL-2

< span> 182 nM (IC 50 )

[IC 50]

IL-4; IL-5; IL-2: 182 nM (IC50)
[storage]

Store at -20°C
[References]

[1] Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug 10;43(16):2975-81. DOI:10.1021/jm990615a
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