NFAT-Transcription-Factor-Regulator-1 - Interleukin Related 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENFAT Transcription Factor Regulator-1Cat. No.: HY-112778CAS No.: 245747-71-1分式: CHFNO分量: 416.28作靶點(diǎn): Interleukin Related作通路: Immunology/Inflammation儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) D

2、MSO : 150 mg/mL (360.33 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.01 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.01 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 NFAT Transcription Factor Regulat

3、or-1是IL-2 合成 的抑制劑，IC50 值為182 nM。IC50 & Target IC50: 182 nM (IL-2 synthesis) 1體外研究 NFAT Transcription Factor Regulator-1 (compound example 19) inhibits IL-2 synthesis with an IC50 of 182nM. NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC50s of 82 and146 nM, res

4、pectively. NFAT Transcription Factor Regulator-1 is able to inhibit IL-4 and IL-5 production inhuman T-cell lines with similar potency to its effects on IL-2 release 1.體內(nèi)研究 NFAT Transcription Factor Regulator-1 is found to have an inhibitory potency approximately 10-fold betterthan that of cyclospor

5、ine. Comparable inhibitory effects on T-cell IL-2 production are obtained with NFATTranscription Factor Regulator-1 and cyclosporine at doses of 3.0 and 30 mg/kg, po, respectively. Theefficacies achieved in monkeys in vivo for blocking T-cell cytokine production suggest that NFATTranscription Factor

6、 Regulator-1 has potential similar to that of cyclosporine for use in transplantation 1.PROTOCOLAnimal Monkey 1Administration 1 Cynomolgus monkeys are bled to obtain heparinized baseline samples for measuring predrug cytokineproduction and then briefly intubated for intragastric dosing. Cyclosporine

7、 is administered in the Neoralformulation. Compound 19 is given. Postdrug blood samples are similarly obtained 2 h later. The samplesare stimulated by spiking undiluted blood with PMA (50 ng/mL) and ionomycin (1g/mL) and incubating for 24h. Plasma samples are collected by centrifugation, and IL-2 co

8、ncentrations are determined by ELISA usingrecombinant human IL-2 as standard 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug10;43(16):2975-81.McePdfHeightCaution: Product has not been fully validated for medical applicatio