2. Immunology/Inflammation
  3. Thrombopoietin Receptor
  4. Avatrombopag

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

目录号: HY-13463 纯度: 99.83%
COA 产品使用指南

摩尔计算器

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。

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Avatrombopag Chemical Structure

Avatrombopag Chemical Structure

CAS No. : 570406-98-3

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规格 价格 是否有货 数量
1 mg ￥750
In-stock
5 mg ￥1500
In-stock
10 mg ￥2400
In-stock
25 mg ￥4775
In-stock
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100 mg 现货 询价
500 mg 现货 询价
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Customer Review

Other Forms of Avatrombopag:

Avatrombopag 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2][3].

IC50 & Target

EC50: 3.3 nM (TPO receptor)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Caco-2 CC50
20.86 μM
Compound: AVATROMBOPAG
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
Caco-2 IC50
5.71 μM
Compound: AVATROMBOPAG
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
体外研究
(In Vitro)

Avatrombopag (E5501；AKR-501) 与重组人 TPO (rhTPO) 一样，特异性靶向 TPO 受体，并在巨核细胞的发育和成熟过程中刺激巨核细胞生成[1]。
Avatrombopag (0 -100 nM) 以浓度依赖性方式支持表达 TPO 受体的 Ba/F3 细胞的增殖。Avatrombopag (0-3 μM) 在细胞中诱导 STAT3 和 STAT5 的酪氨酸磷酸化，以及 ERK 的苏氨酸磷酸化，rhTPO[1] 也是如此。
Avatrombopag 呈浓度依赖性促进人 CB 巨核细胞集落形成CD34+ 细胞。Avatrombopag 的 EC50 为 25 nM，Avatrombopag 的最大活性与 rhTPO[1] 相似。

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

Avatrombopag 相关抗体:

Cell Proliferation Assay[1]

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[1]

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；口服；每日一次，持续 14 天) 增加移植了人 FL CD34+ 细胞的 NOD/SCID 小鼠的人血小板数量[1]。

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)[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

649.65

Formula

C29H34Cl2N6O3S2
CAS 号
性状

固体

颜色

White to off-white

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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 8.33 mg/mL (12.82 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Avatrombopag 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5393 mL 7.6965 mL 15.3929 mL 38.4823 mL
5 mM 0.3079 mL 1.5393 mL 3.0786 mL 7.6965 mL
10 mM 0.1539 mL 0.7696 mL 1.5393 mL 3.8482 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Avatrombopag570406-98-3AKR-501 E5501 YM477AKR501AKR 501E5501E 5501E-5501YM477YM 477YM-477Thrombopoietin ReceptormimicTPOmegakaryocytopoiesismegakaryocytesphosphorylationproliferationNOD/SCIDInhibitorinhibitorinhibit

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目录号：
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