[N-{4-[3,5-bis(Trifluoromethyl)-1H-pyrazol-1-yl]phenyl}-4-methyl-1,2,3-thiadiazole-5-carboxamide] Solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable analog of 3,5-bis(trifluoromethyl)pyrazole (BTP) that specifically inhibits CRAC-mediated calcium influx in T-cells with an IC50 about 10 nM and displays ~31-fold greater selectivity over VOC. Blocks the calcium-induced activation and translocation of nuclear factor of activated T-cells (NFAT). Does not affect the activation of NF-kB and AP-1. Potently inhibits cytokine production (IC50 = 1.7 µM for IL-2) and PBMC proliferation (IC50 = 190 nM). Purity: ≥95% by HPLC. Ref.: Logie, L., et al. 2007. Diabetes In press. Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 5370. Yonetoku, Y., et al. 2006. Bioorg. Med. Chem. 14, 4750. Zitt, C., et al. 2004. J. Biol. Chem. 279, 12927. Trevillyan, J.M., et al. 2001. J. Biol. Chem. 276, 48118. Djuric, S.W., et al. 2000. J. Med. Chem. 43, 2975. |
