NFAT Transcription Factor Regulator-1_product_DataBase

Bioactivity

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

Invitro

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[1].

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].

Name

NFAT Transcription Factor Regulator-1

CAS

245747-71-1

Formula

C17H10F6N4O2

Molar Mass

416.28

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

NFAT Transcription Factor Regulator-1

CAS: 245747-71-1 F: C17H10F6N4O2 W: 416.28