Apixaban Research Grade Compound (Factor Xa Inhibitor) Supplier — UPOR Biotech
Apixaban — a potent, oral, direct, reversible and highly selective factor Xa (FXa) inhibitor (CAS 503612-47-3, C₂₅H₂₅N₅O₄, MW 459.50 g/mol). It blocks free and clot-bound FXa together with prothrombinase activity independent of antithrombin III (Ki 0.08 nM), preventing thrombin generation and thrombus development. The defining reference standard for anticoagulant pharmacology, thrombosis and thromboembolism research — Research Grade (RUO) compound from UPOR Biotech.
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Apixaban (CAS 503612-47-3, C₂₅H₂₅N₅O₄, MW 459.50 g/mol) is a potent, oral, direct, reversible and highly selective factor Xa (FXa) inhibitor belonging to the pyrazolopyridine-carboxamide small-molecule class. As a direct FXa inhibitor (referenced as the active pharmaceutical ingredient of the brand product Eliquis), apixaban targets the rate-limiting step of the coagulation cascade — the conversion of prothrombin to thrombin by factor Xa. Critically, it inhibits both free and clot-bound FXa as well as prothrombinase complex activity, and this action is independent of antithrombin III — unlike indirect inhibitors such as enoxaparin or fondaparinux. Mechanistically, apixaban prevents thrombin generation and subsequent thrombus development without directly affecting platelet aggregation. Its pharmacological profile in reference studies is characterized by a human FXa Ki of 0.08 nM (0.17 nM rabbit), an elimination half-life of approximately 12 hours, ~87% plasma protein binding, and primary metabolism via CYP3A4/5 with P-glycoprotein transport. UPOR Biotech supplies apixaban as a high-purity Research Grade (RUO) reference compound for the anticoagulation and thrombosis research community.
UPOR Biotech positions this compound for anticoagulation research, arterial and venous thrombosis models, stroke-prevention studies, coagulation cascade pharmacology, and as an analytical reference standard. Whether for in vitro FXa inhibition assays, ex vivo prothrombinase studies, or LC-MS method development, the compound is provided as a well-characterized single lot with full analytical documentation. Research Use Only (RUO) — not for human diagnostic or therapeutic use. Every shipment is accompanied by a Certificate of Analysis (HPLC purity, heavy metals, residual solvents, identification by HPLC/IR/MS), MSDS, and NMR data. Manufactured and QC-released under ISO 9001, cGMP, and FDA facility registration, with packaging options of 1 g, 5 g, 10 g, and 50 g sealed amber vials.
Apixaban vs Rivaroxaban — Direct Factor Xa Inhibitors Compared
Both apixaban and rivaroxaban are oral, direct, reversible FXa inhibitors occupying the leading edge of anticoagulation pharmacology. In reference studies, apixaban exhibits a lower peak-to-trough fluctuation in plasma concentration and is dosed twice daily, whereas rivaroxaban is administered once daily. Apixaban’s high FXa selectivity, antithrombin-independent mechanism, and predictable PK profile make it the preferred tool in thrombosis models and FXa pharmacology research; the choice between the two is a key experimental design decision in comparative anticoagulation studies.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Apixaban — Research Grade (RUO) — Direct Factor Xa Inhibitor Reference Compound |
| Synonyms | Apixaban; BMS-562247-01; BMS-562247 |
| CAS Number | 503612-47-3 |
| Molecular Formula | C₂₅H₂₅N₅O₄ |
| Molecular Weight | 459.50 g/mol |
| IUPAC Name | 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide |
| Compound Class | Small-molecule direct factor Xa (FXa) inhibitor — pyrazolopyridine-carboxamide |
| Mechanism | Reversible, direct, selective FXa inhibition (Ki 0.08 nM human); inhibits free and clot-bound FXa and prothrombinase activity independent of antithrombin III |
| Enzyme Selectivity | ≥30,000-fold selective for FXa over thrombin and other serine proteases; no direct effect on platelet aggregation |
| Bioactivity | Ki 0.08 nM human FXa; Ki 0.17 nM rabbit FXa |
| Purity (HPLC) | ≥98.0% (area normalization) |
| Appearance | White to off-white crystalline solid |
| Melting Point | ~236–238°C |
| Optical Rotation | Single enantiomer; achiral assay confirmed by chiral HPLC |
| Identification | HPLC (retention match), IR, MS, ¹H-NMR |
| Solubility | DMSO ≥50 mg/mL; sparingly soluble in aqueous buffers |
| Water Content (KF) | ≤0.5% |
| Residual Solvents | Meets ICH Q3C limits |
| Heavy Metals | ≤10 ppm |
| Protein Binding | ~87% plasma protein bound (reference studies) |
| Elimination Half-Life | ~12 h (reference studies) |
| Metabolism | Primarily CYP3A4/5 (O-demethylation, hydroxylation); P-glycoprotein substrate |
| Storage | 2–8°C, protected from light and moisture, sealed amber vial |
| Grade | Research Grade (RUO) |
| Applications | Thrombosis & thromboembolism research; anticoagulant pharmacology; analytical reference standard |
| Certifications | ISO 9001, cGMP, FDA facility registration |
| Packaging | 1 g / 5 g / 10 g / 50 g sealed amber vials |
| Shelf Life | 3 years |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Apixaban
Potent Direct Factor Xa Inhibition — Ki 0.08 nM
Apixaban binds the active site of factor Xa with a human Ki of 0.08 nM — one of the most potent direct FXa inhibitors available — delivering robust, dose-proportional blockade of the rate-limiting step in thrombin generation. Research Grade (RUO) for in vitro anticoagulant pharmacology.
Ki 0.08 nMFree & Clot-Bound FXa / Prothrombinase Blockade
Inhibits both free FXa and clot-bound FXa, together with the prothrombinase complex — the FXa-driven amplification of thrombin generation. This dual targeting distinguishes direct FXa inhibitors from antithrombin-dependent agents in thrombosis research models.
Free + Clot-Bound FXaAntithrombin-Independent Reversible Action
Apixaban acts without requiring antithrombin III and binds reversibly, enabling washout, re-dosing, and time-course studies in hemostasis models. Selectivity is ≥30,000-fold against thrombin, with no direct effect on platelet aggregation.
Antithrombin-Independent≥98% HPLC Purity Reference Standard
Supplied at ≥98.0% purity by HPLC with COA, MSDS, residual-solvents, and heavy-metals data — a fully documented analytical reference standard for LC-MS method development, calibration curves, and quantitative coagulation research.
Reference StandardApplications
Venous Thromboembolism Research
Reference direct FXa inhibitor for deep-vein thrombosis and pulmonary embolism models — thrombus formation, regression, and prophylaxis protocols in vivo.
Arterial Thrombosis & Stroke-Prevention Studies
Arterial occlusion, ischemic stroke, and thromboembolism prevention studies where FXa-mediated thrombin generation drives occlusive thrombus development.
Coagulation Cascade & Prothrombinase Assays
In vitro chromogenic and fluorogenic FXa assays, prothrombinase complex reconstitution, and thrombin-generation testing (TGT) for mechanism studies.
Anticoagulant Pharmacokinetics
Dose-response, half-life, and CYP3A4/P-gp interaction profiling — reference PK data for comparative anticoagulant pharmacology and drug-drug interaction research.
Hemostasis Model Development
Thrombus weight, bleeding-time, and clot-bound FXa models that distinguish direct from antithrombin-dependent anticoagulant action in hemostasis research.
Analytical Reference Standard & Method Development
Calibration standard for LC-MS/MS bioanalysis, dissolution, and impurity profiling — lot-documented ≥98% purity for quantitative coagulation research.
Frequently Asked Questions
Apixaban is a potent, oral, direct, reversible, highly selective factor Xa (FXa) inhibitor — a pyrazolopyridine-carboxamide small molecule (CAS 503612-47-3, C₂₅H₂₅N₅O₄, MW 459.50 g/mol). It inhibits free and clot-bound FXa and prothrombinase activity independent of antithrombin III, with a human Ki of 0.08 nM. By blocking FXa — the rate-limiting step of the coagulation cascade — apixaban prevents thrombin generation and thrombus development without directly affecting platelet aggregation.
Both are oral, direct, reversible FXa inhibitors, but reference studies show distinct profiles: apixaban has a lower peak-to-trough fluctuation and is administered twice daily, whereas rivaroxaban is once daily. Apixaban also demonstrates high selectivity for FXa with minimal off-target serine protease inhibition. In anticoagulation research, the choice affects dosing schedules, exposure modeling, and study design for thrombosis models.
Apixaban is widely used in venous thromboembolism research, arterial thrombosis and stroke-prevention studies, coagulation cascade and prothrombinase assays, anticoagulant pharmacokinetics, hemostasis model development, and as an analytical reference standard for LC-MS method development. It is the reference direct FXa inhibitor for investigating thrombin generation, thrombus formation, and anticoagulant pharmacology.
Store apixaban at 2–8°C, protected from light and moisture, in the original sealed amber vial. For assays, prepare DMSO stock solutions (≥50 mg/mL) and dilute to working concentrations in aqueous buffer immediately before use. Avoid repeated freeze-thaw cycles. Handle as a pharmaceutical-grade research compound with appropriate personal protective equipment. UPOR Biotech’s apixaban has a 3-year shelf life under recommended storage.
Every shipment includes a Certificate of Analysis (HPLC purity ≥98.0%, heavy metals ≤10 ppm, residual solvents, water content, identification by HPLC/IR/MS/NMR), MSDS, and lot-specific analytical data. Production and QC are conducted under ISO 9001, cGMP, and FDA facility registration. The compound is supplied as Research Grade (RUO) — Research Use Only, not for human diagnostic or therapeutic use.