Avatrombopag hydrochloride

CAS: 570403-17-7 货号: A656441 分子式: C29H35Cl3N6O3S2 分子量: 686.12 PubChem CID: 87588882
有货
级别和纯度: 10mM in DMSO
储存条件
干燥,-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
A656441-1ml
期货 Stock Image
¥5,286.90
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为什么选择此级别

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储存与运输

干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist ( EC 50 =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 .

In Vitro

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 EC 50 is 25 nM for Avatrombopag hydrochloride and the maximum activity of Avatrombopag hydrochloride is similar to that of rhTPO. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

规格

别名
盐酸阿伐曲波帕
规格或纯度
10mM in DMSO
英文名称
Avatrombopag hydrochloride
生化机理
阿伐曲波帕(AKR-501)盐酸盐是一种口服活性非肽促血小板生成素(TPO)受体激动剂(EC 50 =3.3 nM)。阿伐曲博帕格盐酸盐可模拟 TPO 的生物活性。阿伐曲波帕格盐酸盐可通过以下途径增加血小板生成
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CCC(CC1)N2CCN(CC2)C3=C(N=C(S3)NC(=O)C4=CC(=C(N=C4)N5CCC(CC5)C(=O)O)Cl)C6=CC(=CS6)Cl.Cl
PubChem CID
分子量
686.12

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