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首页 / 抑制剂/激动剂 / 免疫/炎症 / 血小板生成素受体 / Avatrombopag

阿伐曲泊帕 /Avatrombopag {[allProObj[0].p_purity_real_show]}

货号：A645681 同义名： YM477;AKR-501

Avatrombopag是一种口服活性的血小板生成素（TPO）受体激动剂，EC50值为3.3 nM。

Avatrombopag 化学结构 CAS号：570406-98-3
Avatrombopag 化学结构
CAS号：570406-98-3
Avatrombopag 3D分子结构
CAS号：570406-98-3
Avatrombopag 化学结构 CAS号：570406-98-3
Avatrombopag 3D分子结构 CAS号：570406-98-3
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Avatrombopag 纯度/质量文件 产品仅供科研

货号：A645681 标准纯度： {[allProObj[0].p_purity_real_show]}
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Avatrombopag 生物活性

描述 Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist with an EC50 of 3.3 nM. It mimics the biological activities of TPO, stimulating platelet production by activating the intracellular signaling system and promoting the generation of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag is metabolized by cytochrome P450 (CYP) 2C9 and CYP3A enzymes [1][2][3].
体内研究

Avatrombopag (0.3-3 mg/kg; pO.; daily for 14 days) enhances human platelet count in NOD/SCID mice that have been transplanted with human FL CD34+ cells [1].
体外研究

Avatrombopag (E5501; AKR-501) selectively binds to the TPO receptor and induces megakaryocytopoiesis during the development and maturation of megakaryocytes, akin to the effect of recombinant human TPO (rhTPO) [1].

Avatrombopag (0-100 nM) promotes the proliferation of Ba/F3 cells expressing the TPO receptor in a concentration-dependent manner. Furthermore, Avatrombopag (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, as well as threonine phosphorylation of ERK in these cells, similar to the effects observed with rhTPO [1].

Avatrombopag induces concentration-dependent formation of megakaryocyte colonies from human CB CD34+ cells. The EC50 for Avatrombopag is 25 nM, and its maximum activity is comparable to that of rhTPO [1].

Avatrombopag 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.

Avatrombopag 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.70mL

1.54mL

0.77mL

15.39mL

3.08mL

1.54mL

Avatrombopag 技术信息

CAS号570406-98-3
分子式C29H34Cl2N6O3S2
分子量 649.655
别名 YM477;AKR-501;AS 1670542;E5501
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C
溶解方案

DMSO: 7 mg/mL(10.77 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Avatrombopag | 570406-98-3 | AKR-501 | E5501 | TPO Receptor Agonist | Immunology/Inflammation | Thrombopoietin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Avatrombopag 纯度/质量文件 | Avatrombopag 生物活性 | Avatrombopag 参考文献 | Avatrombopag 实验方案 | Avatrombopag 技术信息

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