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Avatrombopag

SKU: orb1220399

Description

Avatrombopag is a new oral thrombopoietin (TPO) receptor agonist activating TPO receptor and increasing megakaryocytic proliferation/differentiation and platelet production.(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.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 didrhTPO.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.(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.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Avatrombopag

Key Properties

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CAS Number570406-98-3
MW649.65
Purity>98% (HPLC)
FormulaC29H34Cl2N6O3S2
SMILESO=C(Nc1nc(-c2cc(Cl)cs2)c(N2CCN(C3CCCCC3)CC2)s1)c1cnc(N2CCC(C(=O)O)CC2)c(Cl)c1
TargetTPO
SolubilityDMSO:32 mg/mL (49.26 mM)

Bioactivity

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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. Animal model: NOD/SCID mice (transplanted with human FL CD34+cells). 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.
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. 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. 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. T Cell Proliferation Assay 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. 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.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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AKR-501 | E5501 | YM477

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Quick Database Links

Gene Symbol
TPO

Protocol Information

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Available Sizes

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1 g
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2 mg
$ 150.00
5 mg
$ 210.00
10 mg
$ 320.00
25 mg
$ 570.00
50 mg
$ 930.00
100 mg
$ 1,320.00
500 mg
$ 2,660.00
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