Art. -Nr.: HY-13463

Avatrombopag

(Synonyms: AKR-501; E5501; YM477)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

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.

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Reinheit: 99.83%
CAS. Nr.: 570406-98-3
Formel: C₂₉H₃₄Cl₂N₆O₃S₂
Molecular Weight:649.65

Speicherung:

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

Avatrombopag Chemical Structure

CAS. Nr.: 570406-98-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 3.3 nM (TPO receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	3.3 nM Compound: Avatrombopag	Induction of cell proliferation of mouse BaF3 cells expressing full-length human TPO receptor by WST-1/1-methoxy PMS assay Induction of cell proliferation of mouse BaF3 cells expressing full-length human TPO receptor by WST-1/1-methoxy PMS assay	[PMID: 36758304]
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

In Vitro

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^[1].
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^[1].
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^[1].

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

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 (0.3-3 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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 570406-98-3
Appearance Solid
Molecular Weight 649.65
Formel C₂₉H₃₄Cl₂N₆O₃S₂
Color White to light yellow
SMILES

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

AKR-501; E5501; YM477
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (5)

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Journal Impact Factor

Nature

Chemically defined cytokine-free expansion of human haematopoietic stem cells. [Abstract]

2023 Mar;615(7950):127-133. PMID: 36813966
J Clin Invest

Eltrombopag inhibits TET dioxygenase to contribute to hematopoietic stem cell expansion in aplastic anemia. [Abstract]

2022 Feb 15;132(4):e149856. PMID: 35085104
Eur J Pharmacol

The immune thrombocytopenia therapeutic Avatrombopag alleviates osteoporosis by targeting NFATc1 signaling. [Abstract]

2026 Jan 10:1010:178377. PMID: 41297758
J Thromb Haemost

Generation of a thrombopoietin-deficient thrombocytopenia model in zebrafish. [Abstract]

2022 Aug;20(8):1900-1909. PMID: 35622056
bioRxiv

2025 Sep 13.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 8.33 mg/mL (12.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (477 KB)
- English - EN (477 KB)
- Français - FR (477 KB)
- Deutsch - DE (477 KB)
- Norwegian - NO (477 KB)
- Español - ES (477 KB)
- Swedish - SV (477 KB)
- Italian - IT (477 KB)
- Korean - KR (477 KB)
- Portuguese - PT (477 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. 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]

[2]. 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]

[3]. 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

Avatrombopag

5 Cited Publications

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Avatrombopag

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Publications Citing Use of MedChemExpress (MCE) Avatrombopag

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Avatrombopag

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Publications Citing Use of MedChemExpress (MCE) Avatrombopag

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Avatrombopag Related Classifications

HY-13463 Related Classifications