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 selectiveT-cell costimulationblocker. Belatacept binds toCD 80/86ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants[1]. |
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体外研究
(In Vitro) | Belatacept (0-5 mg/mL, 1 h) inhibits T-cell proliferation in a dose-dependent manner[2].
Belatacept (500 ng/mL, 7 days) enhances predominance of effector-memory T-cells after allogeneic stimulation[2].
Belatacept (100, 500 ng/mL, 7 days) has no effect on differentiation and allogeneic IFNγ production of isolated effector-memory T cells[2].
Belatacept (10 μg/mL, 1 h) does not inhibit follicular T Cell-dependent B-Cell differentiation[4].
Belatacept (40 μg/mL, 10 days) reduces plasmablast differentiation, Ig production, and the major transcription factor Blimp-1 in a T cell-independent manner[5].
Belatacept (40 μg/mL, 30 min) induces activation of the STAT3 transcription factor in stimulated B cells and reduced the expression of CD86[5].
Cell Viability Assay[2] | Cell Line: | PBMCs from healthy volunteers | | Concentration: | 0-5 mg/mL | | Incubation Time: | 1 h | | Result: | Inhibited T-cell proliferation l with IC50values of 215 ng/mL, and residual T-cell proliferation (±30%) was still present at high doses. |
Western Blot Analysis[5] | Cell Line: | CD40L and IL-21 stimulated B cells | | Concentration: | 40 μg/mL | | Incubation Time: | 15, 30 min | | Result: | Increased in STAT signaling determined by increased STAT3 phosphorylation. |
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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[3].
Belatacept (intravenous injection, 20 mg/kg) displays immunosuppressive activities in monkeys immunized with sheep red blood cell[6].
| Animal Model: | Acute rejection model of orthotopic kidney transplantation in rats[3] | | Dosage: | 60 mg/kg | | Administration: | Intraperitoneal injection, at postoperative and 4 days after transplantation. | | Result: | Inhibited creatinine increase after kidney transplantation (combined with BTLA overexpression therapy).
Reduced C4d in graft IF staining, and reduced CD138 infiltration and DSA production. |
| Animal Model: | Rhesus monkeys immunized with sheep red blood cell[6] | | Dosage: | Intra-operatively 10 mg/kg, on day 4 (15 mg/kg) and on post-operative days 14, 28, 42, 56, 70 (20 mg/kg). | | Administration: | intravenous injection | | Result: | Caused a 50% reduction in the peak anti-SRBC response.
Prolonged renal allograft survival and synergies with conventional immunosuppression. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Store at 4°C, do not freeze |
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