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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/阿伐曲泊帕 {[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/阿伐曲泊帕 化学结构 CAS号：570406-98-3
Avatrombopag/阿伐曲泊帕 化学结构
CAS号：570406-98-3
Avatrombopag/阿伐曲泊帕 3D分子结构
CAS号：570406-98-3
Avatrombopag/阿伐曲泊帕 化学结构 CAS号：570406-98-3
Avatrombopag/阿伐曲泊帕 3D分子结构 CAS号：570406-98-3
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Avatrombopag/阿伐曲泊帕 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/阿伐曲泊帕 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/阿伐曲泊帕 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/阿伐曲泊帕 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/阿伐曲泊帕 技术信息

CAS号570406-98-3
分子式C29H34Cl2N6O3S2
分子量 649.65
SMILES Code O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O
MDL No. MFCD18633249
别名 YM477; AKR-501; AS 1670542; E5501
运输蓝冰
InChI Key OFZJKCQENFPZBH-UHFFFAOYSA-N
Pubchem ID 9852519
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

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/阿伐曲泊帕 纯度/质量文件 | Avatrombopag/阿伐曲泊帕 生物活性 | Avatrombopag/阿伐曲泊帕 参考文献 | Avatrombopag/阿伐曲泊帕 实验方案 | Avatrombopag/阿伐曲泊帕 技术信息

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