Avatrombopag
Avatrombopag Basic information
- Product Name:
- Avatrombopag
- Synonyms:
-
- Avatrombopag Base,Avatrombopag
- Avatrombopag (AKR-501)
- AVATROMBOPAG
- AS 1670542
- E 5501
- 4-Piperidinecarboxylic acid, 1-[3-chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-
- Avatrombopag(AS1670542)
- Crenolanib Besylate
- CAS:
- 570406-98-3
- MF:
- C29H34Cl2N6O3S2
- MW:
- 649.65
- EINECS:
- 1312995-182-4
- Product Categories:
-
- Intermediate
- API
- Mol File:
- 570406-98-3.mol
Avatrombopag Chemical Properties
- Density
- 1.440
- storage temp.
- Storage temp. 2-8°C
- solubility
- DMSO:27.33(Max Conc. mg/mL);42.07(Max Conc. mM)
- form
- A crystalline solid
- pka
- 3.04±0.70(Predicted)
- color
- White to off-white
- InChIKey
- OFZJKCQENFPZBH-UHFFFAOYSA-N
- SMILES
- N1(C2=NC=C(C(NC3=NC(C4SC=C(Cl)C=4)=C(N4CCN(C5CCCCC5)CC4)S3)=O)C=C2Cl)CCC(C(O)=O)CC1
Avatrombopag Usage And Synthesis
Description
Avatrombopag is a medication that used for certain conditions that lead to thrombocytopenia (low platelets) such as thrombocytopenia associated with chronic liver disease in adults who are to undergo a planned medical or dental procedure.It was the third thrombopoietin receptor agonist approved for the treatment of immune thrombocytopenia and the first approved to treat periprocedural thrombocytopenia in patients with chronic liver disease (thereby providing an alternative to blood transfusions for these patients). Avatrombopag was approved for medical use in the United States in 2018, and in the European Union in 2019.
Uses
Avatrombopag is used to treat thrombocytopenia (a low number of platelets [type of blood cell needed for blood clotting]) in people with chronic (ongoing) liver disease. It is also used to treat thrombocytopenia in people with chronic immune thrombocytopenia (ITP; an ongoing condition that may cause unusual bruising or bleeding due to an abnormally low number of platelets in the blood).
Mechanism of action
Avatrombopag is in a class of medications called thrombopoietin (TPO) receptor agonists. It works by causing the body to produce more platelets.
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].
| 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. |
target
TPO receptor
IC 50
IC 50 value is 3.3 nM.
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