【产品介绍】：

产品名称 他克莫司 英文名称 Tacrolimus 规格或纯度 分析标准品,≥98% 别名 FK-506 monohydrate 英文别名 FK-506 monohydrate 运输条件 超低温冰袋运输 生化机理 Description:IC50 Value: 0.47 nM (Inhibition of lymphocyte proliferation) [1]Tacrolimus is a potent immunosuppressive drμg often administered to transplant recipient patients and exhibits a variety of adverse cardiovascular effects.in vitro: MP and tacrolimus decreased the number of circulating helper-T cells with IC50 values of 23 ng/ml for MP and 6.7 ng/ml for tacrolimus. After coadministration of these drμgs, an interaction occurs, but the nature (additive or antagonistic) of this interaction was not clear. The IC50 of tacrolimus for in vitro inhibition of lymphocyte proliferation was 0.39 ng/ml (0.47 nM) and 1.02 ng/ml (2.73 nM) for MP. The maximum percentage of inhibition was 94.6% for tacrolimus and 64.9% for MP [1]. K506 inhibited the proliferation of T cell clones stimulated with specific antigens in a dose-dependent manner, and at about 100-fold lower concentrations than CsA. FK506 inhibited both IL-2 secretion and IL-2 receptor expression of BC.21 after stimulation with the specific antigen. FK506 also inhibited the proliferation of BC.21 stimulated with phorbol 12-myristate 13-acetate plus calcium ionophore [2].in vivo:  Rat kidney TAC concentrations were higher (range 109-190 pg/mg tissue) than those in the liver (range 22-53 pg/mg of tissue), with median tissue/blood concentrations ratios of 72.0 and 17.6, respectively. In 2 transplant patients, kidney TAC concentrations ranged from 119 to 285 pg/mg of tissue and were approximately 20 times higher than whole blood troμgh TAC concentrations [3].Clinical trial: PK Tacrolimus in Transplants. Phase 4 .Immunosuppressant. Complexes with FKBP-12 to inhibit calcineurin.CAS编号 104987-11-3 储存温度 -20°C储存 RTECS KD4201200 密度 1.19 分子量 804.02 分子式 C44H69NO12 PubChem CID 445643