Avatrombopag hydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

570403-17-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议

产品名称

AKR-501 hydrochloride
E5501 hydrochloride
YM477 hydrochloride

产品介绍

Avatrombopag (AKR-501) hydrochloride 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 hydrochloride 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 hydrochloride 是细胞色素 P450 (CYP) 2C9 和 CYP3A 的底物。

生物活性

Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptidethrombopoietin (TPO) receptoragonist (EC₅₀=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 ofcytochrome P450(CYP) 2C9 and CYP3A^[1]^[2]^[3].

体外研究
(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^[1].
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^[1].
Avatrombopag hydrochloride promotes megakaryocyte colony formation from human CB CD34⁺cells in a concentration-dependent fashion. The EC₅₀is 25 nM for Avatrombopag hydrochloride and the maximum activity of Avatrombopag hydrochloride is similar to that of rhTPO^[1].

体内研究
(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^[1].

Animal Model:	NOD/SCID mice (transplanted with human FL CD34+cells)^[1]
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.

Clinical Trial

分子量

686.12

性状

Solid

Formula

C₂₉H₃₅Cl₃N₆O₃S₂

CAS 号

570403-17-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 8.33 mg/mL(12.14 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.4575 mL	7.2874 mL	14.5747 mL
5 mM	0.2915 mL	1.4575 mL	2.9149 mL
10 mM	0.1457 mL	0.7287 mL	1.4575 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 0.83 mg/mL (1.21 mM); Clear solution
此方案可获得 ≥ 0.83 mg/mL (1.21 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在本网站选购。