NFAT Inhibitor (cell-permeable

一种可穿透细胞的NFAT抑制剂；在50或100µM剂量下抑制LPS和IFN-γ诱导的小鼠BMDM中的IL-12p40和NO生成；在1mg/kg剂量下防止糖尿病肾病db/db小鼠模型中的肾脏重量和尿白蛋白水平增加；在卵巢切除术诱发的骨质疏松症大鼠模型中，在骨折后16周内，在100µg/kg剂量下改善骨折愈合；在吡罗昔康诱发的结肠炎模型中，在IL-10敲除小鼠中，在1mg/kg剂量下降低病情严重程度。A cell-permeable form of NFAT inhibitor; inhibits IL-12p40 and NO production in LPS- and IFN-γ-induced mouse BMDMs at 50 or 100 µM; prevents increases in kidney weight and urine albumin levels in a db/db mouse model of diabetic nephropathy at 1 mg/kg; improves fracture healing in a rat model of ovariectomy-induced osteoporosis at 100 µg/kg for 16 weeks post-fracture; decreases disease severity in IL-10 knockout mice in a model of piroxicam-induced colitis at 1 mg/kg.分子式C147H259N67O36S • XCF3COOH分子量3573.1O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(NCC(NCC(NCC(N[C@@H](CCSC)C(N[C@H](C(NCC(N1CCC[C@H]1C(N[C@@H](CC2=CNC=N2)C(N3CCC[C@H]3C(N[C@@H](C(C)C)C(N[C@@](C(N[C@@H](C(C)C)C(N[C@@](C(N[C@]([C@H](O)C)([H])C(NCC(N4CCC[C@H]4C(N[C@@H](CC5=CNC=N5)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC=O)C(O)=O)=O)=O)=O)=O)=O)=O)([H])[C@@H](C)CC)=O)=O)([H])[C@@H](C)CC)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(N)=N)N[H].FC(F)(C(O)=O)F