Avatrombopag - CAS:570406-98-3

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Avatrombopag (Synonyms:AKR-501; E5501; YM477)

目录号 : KM8867 CAS No. : 570406-98-3

Data Sheet 产品使用指南

Avatrombopag (AKR-501) 是一种口服活性的非肽血小板生成素受体 (TPO receptor)激动剂 (EC₅₀=3.3 nM)。Avatrombopag 可模拟 TPO 的生物活性。Avatrombopag hydrochloride 通过激活细胞内信号传导系统来增加血小板的产生，并促进造血前体细胞产生血小板和巨核细胞。Avatrombopag是细胞色素 P450 (CYP) 2C9 和 CYP3A 的底物。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC₅₀=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.

体外研究

Avatrombopag (E5501; AKR-501) specifically targets the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as recombinant human TPO (rhTPO) did.
Avatrombopag (0-100 nM) supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion. Avatrombopag (0-3 μM) induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells, as did rhTPO.
Avatrombopag promotes megakaryocyte colony formation from human CB CD34 cells in a concentration-dependent fashion. The EC₅₀ is 25 nM for Avatrombopag and the maximum activity of Avatrombopag is similar to that of rhTPO.

Cell Proliferation Assay

Cell Line:	Ba/F3 cells
Concentration:	0.003 μM, 0.03 μM, 0.3 μM, 3 μM
Incubation Time:
Result:	Increased the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion.

Western Blot Analysis

Cell Line:	Ba/F3 cells
Concentration:	0.003 μM, 0.03 μM, 0.3 μM, 3 μM
Incubation Time:	15 minutes
Result:	Induced tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells.

体内研究

Avatrombopag (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.

分子式

C₂₉H₃₄N₆O₃S₂Cl₂^.C₄H₄O₄

分子量

649.65

CAS号

570406-98-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

DMSO : ≥ 32 mg/mL (49.26 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5393 mL	7.6965 mL	15.3929 mL
5 mM	0.3079 mL	1.5393 mL	3.0786 mL
10 mM	0.1539 mL	0.7696 mL	1.5393 mL

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