Belatacept (BMS 224818) 是一种选择性 T 细胞共刺激 (T-cell costimulation) 阻滞剂。Belatacept 与 CD 80/86 配体结合而抑制 CD-28 介导的 T 细胞共刺激。Belatacept 可用于器官移植免疫抑制的研究。
产品详情
Belatacept (BMS 224818) 是一种选择性 T 细胞共刺激 (T-cell costimulation) 阻滞剂。Belatacept 与 CD 80/86 配体结合而抑制 CD-28 介导的 T 细胞共刺激。Belatacept 可用于器官移植免疫抑制的研究。
生物活性
Belatacept (BMS 224818) is a selective T-cell costimulation blocker. Belatacept binds to CD 80/86 ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants.
性状
Solid
IC50 & Target[1][2]
CD80/86
体外研究(In Vitro)
Belatacept (0-5 mg/mL, 1 h) inhibits T-cell proliferation in a dose-dependent manner.Belatacept (500 ng/mL, 7 days) enhances predominance of effector-memory T-cells after allogeneic stimulation.Belatacept (100, 500 ng/mL, 7 days) has no effect on differentiation and allogeneic IFNγ production of isolated effector-memory T cells.Belatacept (10?μg/mL, 1 h) does not inhibit follicular T Cell-dependent B-Cell differentiation.Belatacept (40?μg/mL, 10 days) reduces plasmablast differentiation, Ig production, and the major transcription factor Blimp-1 in a T cell-independent manner.Belatacept (40?μg/mL, 30 min) induces activation of the STAT3 transcription factor in stimulated B cells and reduced the expression of CD86. has not independently confirmed the accuracy of these methods.
体内研究(In Vivo)
Belatacept (intraperitoneal injection, 60 mg/kg) inhibits ABMR (Antibody-Mediated Rejection), and inhibits acute rejection when combined with BTLA (B and T lymphocyte attenuator) overexpression therapy.
Belatacept (intravenous injection, 20 mg/kg) displays immunosuppressive activities in monkeys immunized with sheep red blood cell. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Store at 4°C, do not freeze
ClinicalTrial
参考文献
[1]. George Melvin, et al. Belatacept: A worthy alternative to cyclosporine?. J Pharmacol Pharmacother. 2012 Jan-Mar; 3(1): 90–92. [2]. Gretchen N de Graav, et al. Down-Regulation of Surface CD28 under Belatacept Treatment: An Escape Mechanism for Antigen-Reactive T-Cells. PLoS One. 2016 Feb 26;11(2):e0148604.
[1]. George Melvin, et al. Belatacept: A worthy alternative to cyclosporine?. J Pharmacol Pharmacother. 2012 Jan-Mar; 3(1): 90–92. [2]. Gretchen N de Graav, et al. Down-Regulation of Surface CD28 under Belatacept Treatment: An Escape Mechanism for Antigen-Reactive T-Cells. PLoS One. 2016 Feb 26;11(2):e0148604.