Avatrombopag AKR-501; E5501; YM477|cas:570406-98-3|西域试剂

Avatrombopag AKR-501; E5501; YM477,99.81%

产品编号：Bellancom-13463| CAS NO：570406-98-3| 分子式：C₂₉H₃₄Cl₂N₆O₃S₂| 分子量：649.65

Avatrombopag(AKR-501;AS1670542)是血小板生成素受体（TPO受体）的新型具口服活性激动剂，EC50值为3.3nM。

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货号	价格	库存与货期
Bellancom-13463	￥3500.00	杭州北京（现货）
Bellancom-13463	￥5000.00	杭州北京（现货）
Bellancom-13463	￥15000.00	杭州北京（现货）
Bellancom-13463	￥21000.00	杭州北京（现货）

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Avatrombopag AKR-501; E5501; YM477

产品介绍

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。

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.

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

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
(In Vivo)

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.

西域 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.

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.

西域 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.

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.

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 8.33 mg/mL (12.82 mM; ultrasonic and warming and heat to 60°C)

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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009;82(4):247-254. [Content Brief]

. 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. [Content Brief]

. 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. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Avatrombopag
CAS号：	570406-98-3
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Avatrombopag
别名：	AKR-501; E5501; YM477
分子式：	C29H34Cl2N6O3S2
分子量：	649.65

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Fukushima-Shintani M, et al. AKR-501 (YM477) a novel orally-active thrombopoietin receptor agonist. Eur J Haematol. 2009 Apr;82(4):247-54.

[2]. Abe M, et al. Pharmacological profile of AS1670542, a novel orally-active human thrombopoietin receptor agonist. Eur J Pharmacol. 2011 Jan 10;650(1):58-63.

Avatrombopag AKR-501; E5501; YM477,99.81%

Avatrombopag AKR-501; E5501; YM477

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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