6-Thioguanosine-5'-O-triphosph

6-硫鸟嘌呤和硫唑嘌呤的活性代谢物；与多种GTP酶结合，但选择性抑制抗CD3和抗CD28抗体刺激的原代人类CD4+T细胞中Rac1和Rac2相对于Cdc42的激活；抑制T细胞受体刺激的T细胞增殖，降低体外分离的小鼠脾细胞中CD28依赖性T细胞存活率；在0.5mg/kg剂量下增加小鼠心脏移植模型中的存活率。An active metabolite of 6-thioguanine and azathioprine; binds to a variety of GTPases but selectively inhibits activation of Rac1 and Rac2 over Cdc42 in primary human CD4+ T cells stimulated with anti-CD3 and anti-CD28 antibodies; inhibits T cell receptor-stimulated proliferation of T cells and reduces CD28-dependent T cell survival in vitro in isolated mouse splenocytes; increases survival in a mouse model of heart transplantation at 0.5 mg/kg.分子式C10H12N5O13P3S • 4Na分子量627.2O[C@@H]1[C@H](O)[C@@H](COP([O-])(OP(OP([O-])([O-])=O)([O-])=O)=O)O[C@H]1N2C=NC3=C2NC(N)=NC3=S.[Na+].[Na+].[Na+].[Na+]