AVATROMBOPAG
Avatrombopag is a research-grade compound used in advanced pharmaceutical and biochemical studies. Chemical & Pharmacological Characteristics The compound is a drug-like, orally active small molecule with high affinity functional agonism at the MPL receptor. In vitro performance depends on receptor expression, serum protein binding, and assay format (cell-based reporter, primary progenitors, or megakaryocyte differentiation). Formulation and solubility control are important to avoid precipitation-driven artifacts. It is primarily applied to investigate compound-specific mechanisms, physicochemical behavior, and analytical or formulation-relevant characteristics under controlled laboratory conditions.
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Product Description
Chemical & Pharmacological Characteristics
The compound is a drug-like, orally active small molecule with high affinity functional agonism at the MPL receptor. In vitro performance depends on receptor expression, serum protein binding, and assay format (cell-based reporter, primary progenitors, or megakaryocyte differentiation). Formulation and solubility control are important to avoid precipitation-driven artifacts.
Mechanism of Action
Avatrombopag activates MPL on megakaryocyte progenitors, promoting downstream JAK2 activation and phosphorylation flow through STAT, MAPK, and PI3K-AKT survival pathways. This increases megakaryocyte maturation signals and supports platelet production outputs in responsive systems.
The mechanistic signature is characterized by enhanced transcriptional programs for proliferation and differentiation, altered cytokine sensitivity, and shifts in apoptosis thresholds in hematopoietic lineages. Experimental designs should distinguish receptor-specific signaling from off-target stress responses by using MPL-negative controls and orthogonal pathway readouts.
Advanced Research Applications
- MPL receptor pathway validation and JAK-STAT signaling modulation studies
- Megakaryocyte differentiation and platelet biogenesis modeling in vitro
- Comparative pharmacology versus other TPO-R agonists (pathway bias profiling)
- Systems biology reconstruction of hematopoietic lineage decisions (omics endpoints)
- Formulation and exposure-response modeling for translational hematology programs
Toxicodynamics & Cellular Hazard Spectrum
- Pro-thrombotic risk signatures in sensitive models; monitor coagulation endpoints
- Liver-related stress signals possible depending on system and exposure duration
- Off-target receptor or transporter interactions at high concentrations; control dosing
- Assay artifacts from solubility limits or aggregation; verify free concentration
- Pathway over-activation may shift differentiation balance; interpret lineage markers carefully
For expert laboratory research only – not intended for biological or therapeutic exposure.
Datasheet
| Molecular Formula | C29H34Cl2N6O3S2 |
|---|---|
| Molecular Weight | 649.7 g/mol |
| CAS Number | 570406-98-3 |
| Storage Condition | Store in a cool, dry place. Keep container tightly closed. Protect from moisture and light. |
| Solubility | Insoluble |
| Purity | Purity information is available upon request (COA). |
| Synonym | AVATROMBOPAG; 570406-98-3; AKR-501; E5501; YM477 |
| IUPAC/Chemical Name | 1-[3-chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)-1,3-thiazol-2-yl]carbamoyl]-2-pyridinyl]piperidine-4-carboxylic acid |
| InChl Key | OFZJKCQENFPZBH-UHFFFAOYSA-N |
| InChl Code | InChI=1S/C29H34Cl2N6O3S2/c30-20-15-23(41-17-20)24-27(37-12-10-35(11-13-37)21-4-2-1-3-5-21)42-29(33-24)34-26(38)19-14-22(31)25(32-16-19)36-8-6-18(7-9-36)28(39)40/h14-18,21H,1-13H2,(H,39,40)(H,33,34,38) |
| References | https://pubchem.ncbi.nlm.nih.gov/compound/9852519; small-molecule |
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