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

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

Cat. No.: HY-13463 Purity: 97.81%
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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.

For research use only. We do not sell to patients.

Avatrombopag Chemical Structure

Avatrombopag Chemical Structure

CAS No. : 570406-98-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 600 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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]

In Vitro

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.
In Vivo

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.
Clinical Trial
Molecular Weight

649.65

Formula

C₂₉H₃₄Cl₂N₆O₃S₂

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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.
References
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Keywords:

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

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Avatrombopag
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