NFAT Transcription Factor Regulator

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Company Name: BOC Sciences  
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NFAT Transcription Factor Regulator manufacturers

NFAT Transcription Factor Regulator Basic information
Product Name:NFAT Transcription Factor Regulator
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-;NFAT Transcription Factor Regulator 1,NFAT Transcription Factor Regulator1;N-(4-(5-(Difluoromethoxy)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide;NFAT Transcription Factor Regulator-1, 10 mM in DMSO
CAS:245747-71-1
MF:C17H10F6N4O2
MW:416.28
EINECS:
Product Categories:
Mol File:245747-71-1.mol
NFAT Transcription Factor Regulator Structure
NFAT Transcription Factor Regulator Chemical Properties
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
pka9.85±0.70(Predicted)
color Light yellow to yellow
Safety Information
MSDS Information
NFAT Transcription Factor Regulator Usage And Synthesis
UsesNFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
Biological ActivityNFAT 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 50IL-4; IL-5; IL-2: 182 nM (IC50)
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
NFAT Transcription Factor Regulator Preparation Products And Raw materials
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