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• 产品描述： Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A

• 靶点： EC50: 3.3 nM (TPO receptor);Thrombin;ThrombopoietinReceptor

• 体外研究：
  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. 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.

• 体内研究：
  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 3 mg/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.

• 参考文献：
  1. Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009;82(4):247-254. 2. Xu H, et al. Avatrombopag for the treatment of thrombocytopenia in patients with chronic liver disease. Expert Rev Clin Pharmacol. 2019 Sep;12(9):859-865. 3. Nomoto M, et al. Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs. Br J Clin Pharmacol. 2018;84(5):952-960.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.539 ml	7.696 ml	15.393 ml
  5 mM	0.308 ml	1.539 ml	3.079 ml
  10 mM	0.154 ml	0.77 ml	1.539 ml
  50 mM	0.031 ml	0.154 ml	0.308 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *