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Avatrombopag

CAS No. : 570406-98-3

MCE 站：Avatrombopag

产品活性：Avatrombopag (AKR-501) 是一种口服活性的非肽血小板生成素受体 (TPO receptor)激动剂 (EC₅₀=3.3 nM)。Avatrombopag 可模拟 TPO 的生物活性。Avatrombopag hydrochloride 通过激活细胞内信号传导系统来增加血小板的产生，并促进造血前体细胞产生血小板和巨核细胞。Avatrombopag是细胞色素 P450 (CYP) 2C9 和 CYP3A 的底物。

研究领域：Immunology/Inflammation

作用靶点：Thrombopoietin Receptor

In Vitro: Avatrombopag (E5501; AKR-501) specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did.
Avatrombopag (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as did rhTPO.
Avatrombopag promotes megakaryocyte colony formation from human CB CD34⁺ cells in a concentration-dependent fashion. The EC₅₀ is 25 nM for Avatrombopag and the maximum activity of Avatrombopag is similar to that of rhTPO.

In Vivo: Avatrombopag (0.3-3 mg/kg; p.o.; daily for 14 days) increases the number of human platelets in NOD/SCID mice transplanted with human FL CD34⁺ cells.

相关产品：TPO agonist 1

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