Avatrombopag

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Avatrombopag 是一种新型口服血小板生成素 (TPO) 受体激动剂，可激活 TPO 受体并增加巨核细胞增殖/分化和血小板生成。

Avatrombopag is a new oral thrombopoietin (TPO) receptor agonist activating TPO receptor and increasing megakaryocytic proliferation/differentiation and platelet production.(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 didrhTPO.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.

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. T Cell Proliferation Assay Cell Line:Ba/F3 cells Concentration:0.003 μM, 0.03 μM, 0.3 μM, 3 μM Incubation Time:Result:Increased the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Western Blot Analysis Cell Line:Ba/F3 cells Concentration:0.003 μM, 0.03 μM, 0.3 μM, 3 μM Incubation Time:15 minutes Result:Induced tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells.

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. Animal Model:NOD/SCID mice (transplanted with human FL CD34+cells)Dosage:0.3, 1, and 3mg/kg Administration:P.o.; daily for 14 days Result:Dose-dependently increased the number of human platelets, resulting in approximately a 2.7‐fold increase at 1 mg/kg/d and a 3.0-fold increase at 3 mg/kg/d on day 14 after the start of administration.

AKR-501 | E5501 | YM477

Others

Other Targets

TPO

Cardiovascular Disease

Idiopathic thrombocytopenic purpura

570406-98-3

649.65

C29H34Cl2N6O3S2

>98% (HPLC)

DMSO:32 mg/mL (49.26 mM)

O=C(Nc1nc(-c2cc(Cl)cs2)c(N2CCN(C3CCCCC3)CC2)s1)c1cnc(N2CCC(C(=O)O)CC2)c(Cl)c1

——

(-20℃)

With Ice Pack

≥ 2 years