Avatrombopag maleate
Based on 5 publication(s) in Google Scholar
Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 677007-74-8
- Formula: C33H38Cl2N6O7S2
- Molecular Weight:765.73
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Avatrombopag maleate
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Biological Activity
Avatrombopag (AKR-501) maleate (0.001-1000 nM) promotes the proliferation of Ba/F3 cells expressing TPO receptor in a concentration-dependent manner (EC50: 3.3 nM)[1].
Avatrombopag (AKR-501) maleate (0.003-3 μM, 15 min) induces the phosphorylation of STAT3, STAT5 and ERK in Ba/F3 cells in a concentration-dependent manner[1].
Avatrombopag (AKR-501) maleate (0.01-1000 nM) promotes megakaryocyte colony formation from human CB CD34+ cells in a concentration-dependent manner (EC50: 3.3 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:0.003, 0.03, 0.3, 3 μM
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Incubation Time:15 min
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Result:Up-regulated the protein levels of Phospho-STAT3, Phospho-STAT5 and Phospho-ERK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice transplanted with human FL CD34+ cells (FL CD34+ cells were injected into 9- to 12-week-old NOD/SCID mice through the tail vein after irradiation with 2.4 Gy as two divided doses at intervals of at least 4 h by an X-ray apparatus)[1]
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Dosage:0.3, 1, 3 mg/kg
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Administration:Oral gavage (p.o.), once per day for 14 d
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Result:Increased human platelet count.
Unchanged mouse platelet count.
Chemical Information
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CAS No. 677007-74-8
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Appearance Solid
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Molecular Weight 765.73
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Formula C33H38Cl2N6O7S2
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Color White to off-white
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SMILES
O=C(C1CCN(C2=NC=C(C(NC3=NC(C4=CC(Cl)=CS4)=C(N5CCN(C6CCCCC6)CC5)S3)=O)C=C2Cl)CC1)O.O=C(O)/C=C\C(O)=O
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Synonyms
AKR-501 maleate; E5501 maleate; YM477 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
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
2022 Aug;20(8):1900-1909. PMID: 35622056 -
Solvent & Solubility
DMSO : 175 mg/mL (228.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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;12(9):859-865. [Content Brief]
[3]. Nomoto M, Zamora CA, Schuck E, 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]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 | 1.3059 mL | 6.5297 mL | 13.0594 mL | 32.6486 mL |
| 5 mM | 0.2612 mL | 1.3059 mL | 2.6119 mL | 6.5297 mL | |
| 10 mM | 0.1306 mL | 0.6530 mL | 1.3059 mL | 3.2649 mL | |
| 15 mM | 0.0871 mL | 0.4353 mL | 0.8706 mL | 2.1766 mL | |
| 20 mM | 0.0653 mL | 0.3265 mL | 0.6530 mL | 1.6324 mL | |
| 25 mM | 0.0522 mL | 0.2612 mL | 0.5224 mL | 1.3059 mL | |
| 30 mM | 0.0435 mL | 0.2177 mL | 0.4353 mL | 1.0883 mL | |
| 40 mM | 0.0326 mL | 0.1632 mL | 0.3265 mL | 0.8162 mL | |
| 50 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6530 mL | |
| 60 mM | 0.0218 mL | 0.1088 mL | 0.2177 mL | 0.5441 mL | |
| 80 mM | 0.0163 mL | 0.0816 mL | 0.1632 mL | 0.4081 mL | |
| 100 mM | 0.0131 mL | 0.0653 mL | 0.1306 mL | 0.3265 mL |