产品说明书

Avatrombopag

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Chemical Structure| 570406-98-3 同义名 : YM477;AKR-501;AS 1670542;E5501
CAS号 : 570406-98-3
货号 : A645681
分子式 : C29H34Cl2N6O3S2
纯度 : 98%
分子量 : 649.655
MDL号 : MFCD18633249
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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：
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].
实验方案
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
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.