2. Immunology/Inflammation Metabolic Enzyme/Protease Stem Cell/Wnt MAPK/ERK Pathway JAK/STAT Signaling
  3. Thrombopoietin Receptor Cytochrome P450 ERK STAT
  4. Avatrombopag maleate

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

Cat. No.: HY-13463A Purity: 99.88%
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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.

Avatrombopag maleate Chemical Structure

Avatrombopag maleate Chemical Structure

CAS No. : 677007-74-8

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Based on 3 publication(s) in Google Scholar

Other Forms of Avatrombopag maleate:

Avatrombopag maleate Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 [1][2][3].

In Vitro

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.

Avatrombopag maleate Related Antibodies

Western Blot Analysis[1]

Cell Line: Ba/F3 cells
Concentration: 0.003, 0.03, 0.3, 3 μM
Incubation Time: 15 min
Result: Up-regulated the protein levels of Phospho-STAT3, Phospho-STAT5 and Phospho-ERK.
In Vivo

Avatrombopag (AKR-501) maleate (0.3-3 mg/kg, p.o., once per day for 14 d) increases the number of human platelets in non-obese diabetic/severe combined immunodeficiency (NOD/SCID) mice transplanted with human fetal liver (FL) CD34+ cells in dose-dependent manner[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 (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]
Dosage: 0.3, 1, 3 mg/kg
Administration: Oral gavage (p.o.), once per day for 14 d
Result: Increased human platelet count.
Unchanged mouse platelet count.
Clinical Trial
Molecular Weight

765.73

Formula

C33H38Cl2N6O7S2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3059 mL 6.5297 mL 13.0594 mL
5 mM 0.2612 mL 1.3059 mL 2.6119 mL
View the 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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Avatrombopag maleate Related Classifications

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:

Avatrombopag677007-74-8AKR-501E5501YM477AKR501AKR 501E 5501E-5501YM 477YM-477Thrombopoietin ReceptorCytochrome P450ERKSTATCYPsExtracellular signal regulated kinasesmimicTPOmegakaryocytopoiesismegakaryocytesphosphorylationproliferationNOD/SCIDInhibitorinhibitorinhibit

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