Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
| Molecular Weight | 686.12 |
| CAS Number | 570403-17-7 |
| Solubility (25°C) | DMSO 8.33 mg/mL |
| Storage | 2-8°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Thrombopoietin/Thrombin Products |
|---|
| Desirudin
Desirudin is a thrombin inhibitor that inhibits thrombosis and venous stasis thrombosis.Desirudin can be used in studies related to thrombocytopenia or platelet dysfunction. |
| TP508
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. |
| Succinyl-(Pro58, D-Glu65)-Hirudin (56-65) (sulfated)
Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide, and has high affnity for thrombin than Hirugen, with a KD < 100 nM. |
| Thrombin receptor peptide ligand
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent. |
| Z-Gly-Pro-Arg-4MβNA
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). |
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