Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia[1].
| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 0.1, 0.3, 1, 3 and 10 mg/kg |
| Administration: | Subcutaneous injection and intravenous injection; 0.1-10 mg/kg (C57BL/6 mice, s.c.), 6-60 mg/kg (Sprague Dawley rats, s.c.), 0.4-30 mg/kg (cynomolgus monkeys, s.c.), 10 mg/kg, (cynomolgus monkeys, i.v.); twice weekly for 8 weeks |
| Result: | Dose-dependently increased the level of RBC, hemoglobin and hematocrit in mice, rats and monkeys. |
References:
[1]. Suragani RN, et al. Transforming growth factor-β superfamily ligand trap ACE-536 corrects anemia by promoting late-stage erythropoiesis. Nat Med. 2014 Apr;20(4):408-14.
Luspatercept (0.1-1000 ng/mL) 抑制 A204 细胞中 GDF11 和 GDF8 诱导的 Smad2 和 Smad 3 信号通路[1]。
Luspatcept 与 GDF11，GDF8，activin B，BMP10 和 BMP6 结合[1]。
Luspatercept (0.1-60mg /kg，皮下注射；10mg /kg，静脉注射；每周 2 次，共 8 周) 增加小鼠、大鼠和猴子的红细胞 (RBC) 数量、血红蛋白水平和红细胞堆积[1]。
Luspatercept (10mg /kg，皮下注射，1 次) 降低 C57BL/6 小鼠骨髓和脾脏中的红细胞形成单位 (BFU-Es) 和红血球形成单位 (CFU-Es)[1]。
Luspatercept (10mg /kg，腹腔注射，1 次) 抑制小鼠脾脏 Smad2/3 磷酸化[1]。