产品
编 号：F612181
分子式：C29H35Cl3N6O3S2
分子量：686.12
分子式：C29H35Cl3N6O3S2
分子量：686.12
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
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10mg
询价
询价
50mg
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结构图
CAS No: 570403-17-7
产品详情
生物活性：
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
体内研究：
Avatrombopag hydrochloride (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.
体外研究：
Avatrombopag (E5501; AKR-501) hydrochloride specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did. Avatrombopag hydrochloride is showed to have effect in humans and chimpanzees only.Avatrombopag hydrochloride (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag hydrochloride (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as did rhTPO.Avatrombopag hydrochloride promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent fashion. The EC50 is 25 nM for Avatrombopag hydrochloride and the maximum activity of Avatrombopag hydrochloride is similar to that of rhTPO.
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
体内研究：
Avatrombopag hydrochloride (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.
体外研究：
Avatrombopag (E5501; AKR-501) hydrochloride specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did. Avatrombopag hydrochloride is showed to have effect in humans and chimpanzees only.Avatrombopag hydrochloride (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag hydrochloride (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as did rhTPO.Avatrombopag hydrochloride promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent fashion. The EC50 is 25 nM for Avatrombopag hydrochloride and the maximum activity of Avatrombopag hydrochloride is similar to that of rhTPO.
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