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

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

製品番号: HY-13463 純度: 97.81%
取扱説明書

Avatrombopag (E5501; AKR-501; YM477) is an orally-active thrombopoietin (TPO) receptor agonist with an EC50 value of 3.3 nM and may be useful in the treatment of patients with thrombocytopenia.

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Avatrombopag 構造式

Avatrombopag 構造式

CAS 番号 : 570406-98-3

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 600 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 600 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1800 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2520 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

Avatrombopag (E5501; AKR-501; YM477) is an orally-active thrombopoietin (TPO) receptor agonist with an EC50 value of 3.3 nM and may be useful in the treatment of patients with thrombocytopenia[1].

IC50 & Target

EC50: 3.3 nM (TPO receptor)[1]

体外実験

Avatrombopag (0.003-3 μM; Ba/F3 cells) treatment supports the proliferation of TPO receptor expressing Ba/F3 cell in a concentration-dependent fashion[1].
Avatrombopag (0.003-3 μM; 15 minutes; Ba/F3 cells) treatment induces tyrosine phosphorylation of STAT3 and STAT5, and threonine phosphorylation of ERK in the cells. Avatrombopag activates signal transduction in TPO receptor expressing Ba/F3 cells through the TPO receptor, and supports the proliferation of these cells[1].

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.
体内実験

Avatrombopag (0-3 mg/kg; oral administration; once per day; for 14 days; NOD/SCID mice with human FL CD34+ cells) treatment dose dependently increases the number of human platelets. Withdrawal of Avatrombopag administration causes the human platelet count to return nearly to pretreatment levels[1].

Animal Model: NOD/SCID mice (9-12-week-old) with human FL CD34+ cells[1]
Dosage: 0 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: Oral administration; once per day; for 14 days
Result: Dose dependently increased the number of human platelets.
臨床実験
分子量

649.65

分子式

C₂₉H₃₄Cl₂N₆O₃S₂

CAS 番号

570406-98-3

SMILES

O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 32 mg/mL (49.26 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
参考文献
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Keywords:

AvatrombopagE5501AKR-501YM477E 5501E-5501AKR501AKR 501YM 477YM-477Thrombopoietin ReceptorInhibitorinhibitorinhibit

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製品名:
Avatrombopag
製品番号:
HY-13463
数量:
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